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Intermediate compounds and methods of synthesis of analogues of halichondrin b
Intermediate compounds and methods of synthesis of analogues of halichondrin b
IPC classes for russian patent Intermediate compounds and methods of synthesis of analogues of halichondrin b (RU 2489437):
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FIELD: biotechnologies.

SUBSTANCE: methods are described for synthesis of intermediate compounds used in synthesis of analogues of halichondrin B, in particular, the method to produce substantially diastereomer-pure composition of the compound with the formula including: crystallisation of the specified compound of the formula (I) from the mixture of diastereomers with production of a composition, in which the ratio of the specified compound of the formula (1) to a compound with the opposite stereochemical configuration of chiral centre, indicated with an asterick, makes at least 8:1, where the specified compound of the formula (I) represents: where: z is a single or double link, provided that whenever z is a double link, X2 is C, and Y1 is a hydrogen atom; and provided that when z is a single link, X is CH or O; X1 is O; Y1 is a halogen atom, a hydrogen atom or O-L2, or is absent, when X is O; L1 and L2 independently represent a hydrogen atom or a protective group, or L1 and L2 together are a protective group; or its salt. The invention also includes a whole row of intermediate compounds and a composition of a mixture of separate diastereomers of these compounds.

EFFECT: improved properties of compounds.

75 cl, 15 ex

 

The text descriptions are given in facsimile form.

1. The method of obtaining essentially diastereomers pure compositions of compounds of formula (I), including
crystallization of the compounds of formula (I) from a mixture of diastereoisomers with obtaining a composition in which the ratio of the compounds of formula (I) to the connection with the opposite stereochemical configuration is oracea chiral center, indicated by an asterisk, is at least 8:1, where the aforementioned compound of formula (I) is a

where z represents a single or double bond, provided that when z is a double bond, X2represents s and Y1represents a hydrogen atom; provided that when z represents a single bond, X2represents CH or;
X1represents About;
Y1represents a halogen atom, a hydrogen atom or O-L2or absent when X2represents About;
L1and L2independently represent a hydrogen atom or a protective group, or L1and L2together represent a protective group; or its salt.

2. The method according to claim 1, wherein at least one of L1and L2represents a protective group and is independently selected from C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, C1-C6-alkoxy-(C1-C6)-alkyl or C1-C6-Olkiluoto of ester or L1and L2together form a cyclic C1-C6-acetal, cyclic3-C7-ketal or cyclic carbonate.

3. The method according to claim 1, in which at least Odie the L 1and L2represents a protective group and is independently selected from the group consisting of C1-C6-alkylsilane, C1-C6-alkyl, benzoyl or C1-C8-alkyl substituted carbonyl.

4. The method according to claim 1, wherein at least one of L1and L2represents a protective group, and independently represents methoxymethyl, trimethylsilyl, triethylsilyl, tributylammonium, tertbutylphenol, triisopropylsilyl, methyl, tertbutyl, 3,4-dimethoxybenzyl, p-methoxybenzyl, benzyl or trityl, or L1and L2together form cycloheptylamine.

5. The method according to claim 1, wherein at least one of L1and L2represents a C1-alkylsulphonyl, or L1and L2together form an acetonide, benzylidene, cyclohexylidene or cyclopentolate.

6. The method according to claim 1, in which Y1is a O-L2and L1and L2together form a protective group, which is a4-C7is an alkyl ring with one of the members of the ring covalently associated with both atom in Y1and X1.

7. The method according to claim 1, in which the aforementioned ratio is at least 20:1.

8. The method according to claim 1, in which the indicated compound of formula (I) is a compound of formula (Ib)

where L1aThe L 1bindependently represent a hydrogen atom or a protective group, or L1aand L1btogether represent a divalent protective group.

9. The method according to claim 8, in which each of L1aand L1brepresents a protective group, independently selected from C1-C6of alkyl, aryl(C1-C6)-alkyl, silyl-(C1-C10or C1-C6-Olkiluoto of ester or L1aand L1btogether form a cyclic C1-C6-acetal, cyclic3-C7-ketal or cyclic carbonate.

10. The method according to claim 8, in which the mentioned bivalent protective group is cyclohexylidene protective group.

11. The method according to claim 1, in which the indicated compound of formula (I) selected from the group consisting of

12. The method according to claim 1, in which heptane is present as antibacterial.

13. The method according to item 12, which additionally there is a co-solvent selected from the group consisting of tertbutylamine ether and isopropanol.

14. The method according to claim 1, in which adds the base.

15. The method according to 14, in which the specified radix is trebuchet potassium.

16. The method according to claim 1, in which the specified composition contains a compound of the formula (I) and the compound of formula (Ie) inratio, at least 30:1, and a specified compound of formula (Ie) is:

17. The method of obtaining essentially diastereomers pure compositions of compounds of formula (Ib) of the compounds of formula (Ia),
where the compound of formula (Ia) is a

and the compound of formula (Ib) is a

where L1aand L1bindependently represent a hydrogen atom or a protective group, or L1aand L1btogether represent a divalent protective group, provided that L1ain formulas (Ia) and (Ib) are the same, and L1bin formulas (Ia) and (Ib) are the same, and the method includes
the interaction of the compounds of formula (Ia) in the alkylation conditions with the formation of a mixture containing the compound of formula (Ib) and its diastereomers; and
crystallization of the compounds of formula (Ib) from the mixture to obtain a composition in which the ratio of the compounds of formula (Ib) to connect with the opposite stereochemical configuration of the chiral center marked with an asterisk is at least 8:1.

18. The method according to 17, in which the said alkylation conditions include aprotic solvent, a base and a C1-alkylhalogenide or methylsulfonate.

19. The method according to p in which kazanyarmarka solvent represents tetrahydrofuran, toluene or tertBUTYLPEROXY ether.

20. The method according to 17, in which the specified crystallization involves adding the base.

21. The method according to claim 20, in which the specified radix is diisopropylamide lithium, potassium, hexamethyldisilazane or trebuchet potassium.

22. The method according to 17, in which the aforementioned ratio is at least 20:1.

23. The method according to 17, in which each of L1aand L1brepresents a protective group, independently selected from the group consisting of C1-C6of alkyl, aryl (C1-C6)-alkyl, silyl-(C1-C10and C1-C6-Olkiluoto of ester or L1aand L1btogether form a cyclic C1-C6-acetal, cyclic3-C7-ketal or cyclic carbonate.

24. The method according to 17, in which the mentioned bivalent protective group is cyclohexylidene protective group.

25. The method of obtaining essentially diastereomers pure compositions of compounds of formula (II), including
crystallization of the compounds of the formula (II) from a mixture of diastereoisomers with obtaining a composition in which the ratio of the compounds of the formula (II) to the connection with the opposite stereochemical configuration of the chiral center marked with an asterisk is at least 8:1, where the decree is TES compound of formula (II) is a

where
is a single or double bond, provided that when is a double bond, m is 0 and Y3represents O or CHCO2-L3; provided that when is a single bond, m is 0 or 1 and Y3represents CH2O-L3CH2CO3-L3or CH2CH2O-L3;
Y2represents a C1-C7-sulfonate, O-L4or halogen atom;
L4represents a hydrogen atom or a protective group;
each of the L3and L5independently represents a hydrogen atom or a protective group, or L3and L5together represent a protective group;
or its salt.

26. The method according A.25, in which at least one of L3and L5represents a protective group and is independently selected from C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate or C1-C6-alkoxy-(C1-C6)-alkyl, or L3and L5together form a cyclic C1-C6-acetal, cyclic3-C7-ketal or cyclic carbonate.

27. The method according A.25, where L4represents a protective group selected from C1-C12-alkitab the sludge, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, and C1-C6-alkoxy-(C1-C6)-alkyl.

28. The method according A.25, where L3L4or L5represents a protective group selected from the group consisting of methoxymethyl, trimethylsilyl, triethylsilyl, tributyltinhydride, tertbutylphenol, triisopropylsilyl, methyl, tertbutyl, 3,4-dimethoxybenzyl, p-methoxybenzyl, benzyl and trityl, or L3and L5together form an acetonide, benzylidene, cyclopentolate, cyclohexylidene or cycloheptylamine.

29. The method according A.25, where Y3represents CH2CO2-L3and L3represents a C1-C10-alkyl, C6-C10-aryl-C1-C6-alkyl or C6-C10-aryl.

30. The method according A.25, where L3represents methyl.

31. The method according A.25, where L3and L5together form a cyclic C1-C6-acetal or cyclic With3-C7-ketal.

32. The method according A.25 in which the specified crystallization involves the dissolution of the compounds of formula (II) in a polar solvent.

33. The method according to p, wherein said polar solvent is tertBUTYLPEROXY ether.

34. The method according to p, further comprising prior to the providing of antibacterial.

35. The method according A.25, in which this ratio is at least 20:1.

36. The method according A.25 in which this composition contains a compound of the formula (II) and the compound of formula (IIb) in a ratio of at least 30:1, where the aforementioned compound of formula (IIb) is a

37. The method according A.25, in which the indicated compound of formula (II) is a

Connection AF.

38. The compound of formula (I)

where z represents a single or double bond, provided that when z is a double bond, X2represents s and Y1represents a hydrogen atom; and provided that when z represents a single bond, X2represents CH or;
X1represents About;
Y1represents a halogen atom, a hydrogen atom or O-L2or absent when X2represents O; and
L1and L2independently represent a hydrogen atom or a protective group, independently selected from bentilee, C1-C12alkylcarboxylic, C1-C6alkyl, C1-C15alkylsilanes, aryl (C1-C6) alkyl, C1-C6alkoxy-(C1-C6) alkyl groups and C1-C6Olkiluoto sloneg the ether, or L1and L2together represent a protective group selected from cyclic C1-C6acetal, cyclic3-C7Catala and cyclic carbonate; or its salt.

39. Connection § 38, in which at least one of L1and L2represents a protective group and is independently selected from C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, C1-C6-alkoxy-(C1-C6)-alkyl or C1-C6-Olkiluoto of ester or L1and L2together form a cyclic C1-C6-acetal, cyclic3-C7-ketal or cyclic carbonate.

40. Connection § 38, in which at least one of L1and L2represents a protective group selected from the group consisting of methoxymethyl, trimethylsilyl, triethylsilyl, tributyltinhydride, tertbutylphenol, triisopropylsilyl, methyl, tertbutyl, 3,4-dimethoxybenzyl, p-methoxybenzyl, benzyl and trityl, or L1and L2together form cycloheptylamine.

41. Connection § 38, in which at least one of L1and L2represents a C1-alkylsulphonyl, or L1and L2together form an acetonide, benzylidene, cyclohexylidene or kilometrage.

42. Connection § 38, in which at least one of L1and L2represents a protective group, and represents a C1-C6alkylsilane, C1-C6-alkyl or C1-C8-alkyl substituted carbonyl.

43. Connection § 38, in which Y1is a O-L2; L1and L2together form a protective group, which is a4-C7is an alkyl ring with one of the members of the ring covalently associated with both O Y1and X1.

44. Connection § 38, which is a

45. Connection § 38, which is selected from the group consisting of

46. Connection § 38, which is a compound of formula (Ib)

where L1aand L1bindependently represent hydrogen or a protective group selected from the group consisting of C1-C6-alkyl, aryl-(C1-C6)-alkyl, silyl-(C1-C10and C1-C6-Olkiluoto of ester or L1aand L1btogether form a bivalent protective group selected from the group consisting of cyclic C1-C6-acetal, cyclic3-C7-Catala and cyclic carbonate.

47. Connection § 46, in which each of L1aand L1b represents a protective group, or L1aand L1btogether form a bivalent protective group.

48. Connection § 46, in which the mentioned bivalent protective group is cyclohexylidene protective group.

49. The compound of formula (II):

where
is a single or double bond, provided that when is a double bond, m is 0, and Y3represents O or CHCO2-L3; and provided that when represents a single bond, m is 0 or 1, and Y3represents CH2O-L3CH2CO2-L3or CH2CH2O-L3;
Y2represents a C1-C7-sulfonate, O-L4or halogen atom;
L4represents a hydrogen atom or a protective group selected from the group consisting of C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, and C1-C6-alkoxy-(C1-C6)-alkyl; and
each of the L3and L5independently represents a hydrogen atom or a protective group selected from the group consisting of C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, and C 1-C6-alkoxy-(C1-C6)-alkyl, or L3and L5together represent a protective group selected from the group consisting of cyclic C1-C6-acetal, cyclic3-C7-Catala or cyclic carbonate, or provided that Y3represents CH2CO2-L3L3represents a C1-C10alkyl, C6-C10aryl-C1-C6alkyl or C6-C10aryl; or its salt.

50. Connection § 49, in which at least one of L3and L5represents a protective group and is independently selected from C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate or C1-C6-alkoxy- (C1-C6)-alkyl, or L3and L5together form a cyclic C1-C6-acetal, cyclic3-C6-ketal or cyclic carbonate.

51. Connection § 49, in which L4represents a protective group selected from the group consisting of C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, and C1-C6-alkoxy-(C1-C6)-alkyl.

52. Connection § 49, in which L3L4or L5presented yet a protective group, selected from the group consisting of methoxymethyl, trimethylsilyl, triethylsilyl, tributyltinhydride, tertbutylphenol, triisopropylsilyl, methyl, tertbutyl, 3,4-dimethoxybenzyl, p-methoxybenzyl, benzyl and trityl, or L3and L5together form an acetonide, benzylidene, cyclopentolate, cyclohexylidene or cycloheptylamine.

53. Connection § 49, in which Y3represents CH2CO2-L3and L3represents a C1-C10-alkyl, C6-C10-aryl-C1-C6-alkyl or C6-C10-aryl.

54. Connection § 49, in which L3represents methyl.

55. Connection § 49, in which L3and L5together form a cyclic C1-C6-acetal or cyclic With3-C7-ketal.

56. Connection § 49, in which Y2represents a halogen atom.

57. Connection p, wherein said halogen atom is an atom of iodine.

58. Connection § 49, which is selected from the group consisting of

59. The method of obtaining connection-1939

including making connections AF

in connection EN

the conversion of compounds of the Academy of Sciences in connection A

and transformation connection AI a connection In 1939.

60. The method according to p, in which
(a) compound AF produced from compound AD

or (b) the connection AF get way A.25.

61. The method according to p, in which the connection between AD get the method according to claim 1.

62. The connection, which is a

63. The compound having the formula

Connection AR

64. The compound having the formula

65. A composition comprising a compound having the formula

where z represents a single or double bond, provided that when z is a double bond, X2is, a Y1represents a hydrogen atom, and when z represents a single bond, X2represents CH or;
X1represents O, X2represents About;
Y1represents a halogen atom, a hydrogen atom or O-L2or absent when X2represents About;
L1and L2independently selected from a hydrogen atom and a protective group, or L1and L2together form a protective group;
or its salt.

66. The composition according to p, where the compound has the formula

6. The composition according to p, where the diastereoisomer of the compound has the formula

where L1aand L1bindependently selected from a hydrogen atom and a protective group, or L1aand L1btogether form a bivalent protective group.

68. The composition according to p, where L1aand L1brepresent a protective group which is optionally selected from C1-C6of alkyl, aryl(C1-C6)-alkyl, silyl-(C1-C10and C1-C6Olkiluoto of ester or L1aand L1btogether represent a divalent protective group, which does not necessarily represent cyclic C1-C6acetal, cyclic3-C7ketal, a cyclic carbonate or cyclohexylidene.

69. The composition according to p, where at least one of L1and L2represents a protective group, and independently represents a C1-C12-alkylsulphonyl, C1-C6-alkyl, C1-C15-alkylsilane, aryl-(C1-C6)-alkyl, carbonate, C1-C6-alkoxy-(C1-C6)-alkyl or C1-C6-alkilany ester, or L1and L2together form a cyclic C1-C6acetal, cyclic3-C7ketal or cyclic carbonate.

70. The composition according to p, where at least one of L1and L2 represents a protective group selected from the group consisting of methoxymethyl, trimethylsilyl, triethylsilyl, tributyltinhydride, tertbutylphenol, triisopropylsilyl, methyl, tertbutyl, 3,4-dimethoxybenzyl, parametersbodily, benzyl and trityl, or L1and L2together form cycloheptylamine.

71. The composition according to p, where at least one of L1and L2represents a C1alkylsulphonyl or L1and L2together form an acetonide, benzylidene, cyclohexylidene or cyclopentolate.

72. The composition according to p, where at least one of L1and L2represents a protective group and represents a C1-C6alkylsilane, C1-C6alkyl or C1-C6alkyl substituted carbonyl.

73. The composition according to p, where Y1is a O-L2; L1and L2together form a protective group, which is a4-C7alkyl ring with one of the members of the ring covalently associated with both O Y1and X1.

74. The composition according to p, where the diastereoisomer of compounds selected from

75. Composition according to any one of p-74, where the ratio of the diastereoisomer having the formula

the diastereoisomer having the formula
is at least 8:1, 20:1 or 30:1.

 
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