Derivatives 12,13-amoxicilina and methods for their production

 

(57) Abstract:

Describes new derivatives of 12,13-amoxicilina formula I, where R denotes O, R1represents CHO or CH(OCH3)2, R2denotes H or mikrosil and---- indicates a single bond; or where R represents NOH, R1represents CHO or CH(OCH3)2, R2denotes H or mikrosil and---- denotes a single or double bond; or compounds of formula II, where R denotes H or mikrosil. The compounds exhibit antimicrobial activity. Also describes the methods for their preparation. 2 C. and 15 C.p. f-crystals.

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1) the technical Field to which the invention relates

The present invention relates to a derivative of tylosin, a new synthetic products from the class of macrolides, exhibiting antimicrobial activity. More specifically, the invention relates to a derivative 12,13-amoxicilina formula I

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where R denotes O, R1represents CHO or CH(OCH3)2, R2denotes H or mikrosil and --- represents a single bond; or

where R represents NOH, R1represents CHO or CH(OCH3)2, R2denotes H or mikrosil and---- denotes a single or double bond; and to compounds form CLASS="ptx2">

2) prior art

Have been a number of modifications of the diene part of the 16-membered milasinovic rings. It is known that by the addition of thiols got a simple 11-thioethers tylosin (S. Omura, U.S. patent 4594338). It is also known that the catalytic hydrogenation of diene and aksamitowana in positions C-9 and C-20 tylosin were obtained 10,11,12,13-tetrahydropyrimidine, according to their oximes (A. Naranda, U.S. patent 5023240). It is known that selective oxidation of tylosin allowed to get 12,13-epoxypropane (A. K. Mallams, U.S. patent 4808575). Were also received dihydro - tetrahydropyrimidine other 16-membered macrolides with 12,13-epoxypropoxy. In addition, it is known that catalytic hydrogenation of peridomicile received 13-hydroxy-10,11,12,13-tetrahydropyridine [M. Muroi, Chem. Pharm. Bull. 24 (1976), 450], where the recovery of C10-C11-double bond is carried out by open oxiranes cycle, while catalytic hydrogenation rosamarina got 10,11-dihydroprogesterone preserving 12,13-epoxypropyl. Moreover, it is known that aksamitowana rosamilia and 12,13-epoxypropane were obtained C-20 aldoxime (H. Reinmann, U.S. patent 4056616).

In the existing literature 10,11-dihydroprogesterone 12,13-EPoX the bridge is not described, and nowhere describes how to get mentioned in the present description derivatives of tylosin.

3) the Description of the invention and variants of its implementation

It was found that derivatives 12,13-amoxicilina formula I

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where R denotes O, R1represents CHO or CH(OCH3)2, R2denotes H or mikrosil and---- indicates a single bond; or

where R represents NOH, R1represents CHO or CH(OCH3)2, R3denotes H or mikrosil and---- denotes a single or double bond; and the compounds of formula II

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where R denotes H or mikrosil can be obtained by a method in which the compound of formula III

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A) where R1represents CHO or CH(OCH2)2, R2denotes H or mikrosil and R3denotes N(CH3)2or N-(OCH3)2when R2denotes H; is subjected to hydrogenation in an organic solvent, especially in the lower C1-C3aliphatic alcohol, in the presence of 2-5% wt. palladium on coal under hydrogen pressure of 0.2-0.5 MPa and at room temperature for 5-8 h, after which the compound obtained of the formula I, where R denotes O, R1denotes CH(OCH3)2, R2the seat is of hydroxylaminopurine in pyridine or a lower alcohol with the addition of the base, such as pyridine (or Na2CO3), in a stream of nitrogen at room temperature or at the boiling point under reflux for 3-7 h and then optionally subjected to hydrolysis acetamino group in a mixture of acetonitrile with 0.2 H HCl (1:1) or a mixture of acetonitrile with 1% triperoxonane acid in water (1:2) at room temperature for 2 h; or

B) where R1denotes CH(OCH3)2, R2denotes H or mikrosil and R3denotes N(CH3)2are occimiano, as described above, and the resulting products: compound of formula I, where R denotes NOH, R1denotes CH(OCH3)2, R2denotes H or mikrosil and---- represents a double bond, and the compound of formula II, where R2denotes H or mikrosil, divided by column chromatography on silica gel and acetamino group optionally subjected to hydrolysis described by.

In accordance with the present invention new compounds emit conventional extraction halogenated hydrocarbons such as carbon tetrachloride, chloroform or methylene chloride, in aqueous alkaline solutions and evaporation to a dry residue. If necessary, the selection of the reaction products, 0-230 mesh/ASTH, respectively) in the solvent system methylene chloride/methanol/ammonium hydroxide: A (90:9:1,5) or B (90:9:0,5).

Identification of new compounds made of UV - and NMR-spectroscopy. These new compounds exhibit antibacterial activity and can be used as intermediates in obtaining new derivatives of tylosin. Below the invention is illustrated in the examples which do not limit the scope of the invention.

Example 1

20 dimethylacetal 10,11-dihydro-12,13-amoxicilina (1)

2.4 g (2.4 mmole) of 20-dimethylacetal 12,13-amoxicilina dissolved in 240 ml of ethanol, add to 0.72 g of 10% Pd/C and the mixture hydrogenized at room temperature and a hydrogen pressure of 0.2 MPa for 8 hours After completion of the reaction the catalyst is separated by filtration, the ethanol is evaporated under reduced pressure to obtain a dry product, which is then chromatografic on a column of silica gel.

Yield: 1.25 g (52%), Rf (A): 0,65;

1H-NMR (CDCl3, part./million): 5,10 (1H, d, 1"), 4,58 (1H, d, 1"'), 4,24 (1H, d, 1'), to 3.64 (3H, s, 3"'OMe), 3,51 (3H, s, 2"'OMe), 3,39 (3H, s, 20-OMe), 3,24 (3H, s, 20-OMe), 2,52 (6H, s, NMe2), of 1.34 (3H, s, 12-CH3);

13C-NMR (CDCl3, part./million): 212,31 (s, C-9), 170,48 (s, C-1), 103,27 (d, C-1'), 102,94 (d, C-20), 99,36 (d, C-1"'

Example 2

10,11-dihydro-12,13-apokathilosis (2)

2 g (2.1 mmole) 12,13-amoxicilina dissolved in 200 ml of ethanol, add 0.4 g 10% Pd/C and hydrogenized at room temperature and a hydrogen pressure of 0.4 MPa for 7 hours the Product emit similar to that described in example 1.

Output: 0,92 g (46%), Rf (A): 0,54;

1H-NMR (CDCl3, frequent. /million): 9,67 (1H, s, CHO), 5,09 (1H, d, 1"), 4,58 (1H, d, 1"'), 4,25 (1H, d, 1'), the 3.65 (3H, s, 3"'OMe), 3,50 (3H, s, 2"'OMe), of 2.51 (6H, s, NMe2), of 1.23 (3H, s, 12-CH3);

13C-NMR (CDCl3, frequent. /million): 212,33 (s, C-9), 202,86 (d, C-20), 170,46 (s, C-1), 103,25 (d, C-1'), 99,36 (d, C-1"'), 96,74 (d, C-1'), 60,66 (q, 3"'OMe), 59,29 (s, C-12), 58,37 (q, 2"'OMe; d, C-13), 33,87 (t, C-10), 28,95 (t, C-11), 18,36 (q, C-22).

Example 3

20 dimethylacetal 10,11-dihydro-12,13-epoxidation (3)

How A

2.5 g (2.9 mmole) of N-oxide 20-dimethylacetal 12,13-epoxidation dissolved in 250 ml of ethanol, added to 1.25 g of 10% Pd/C and hydrogenized at room temperature and a hydrogen pressure of 0.5 MPa for 7 o'clock

The product distinguish similar to that described in example 1.

Yield: 1.27 g (52%), Rf (A): 0,57;

1H-NMR (CDCl3, frequent. /million): 4,56 (1H, d, 1"'), 4,25 (1H, d, 1'), to 3.64 (3H, s, 3"'OMe), 3,51 (3H, s, 2"'OMe), to 3.38 (3H, s, 20-OMe), up 3.22 (3H, s, 20-OMe), 2,52 (6H, s, NMe2), of 1.33 (3H, s, 12-CH3);

13C-NMR (CDCl3, part./million): 212,31 (s, C-9), 170,99 (t, C-11), 18,38 (q, C-22).

Method B

3 g (3.6 mmole) of 20-dimethylacetal 12,13-epoxidation dissolved in 250 ml of ethanol, add 0.6 g of 10% Pd/C and hydrogenized at room temperature and a hydrogen pressure of 0.5 MPa for 8 hours, the Product obtained by selection in the same manner as in example 1, identical to the product obtained by method A.

Example 4

10,11-dihydro-12,13-epoxidation (4)

2.4 g (3 mmole) 12,13-epoxidation dissolved in 100 ml of ethanol, add to 0.72 g of 10% Pd/C and hydrogenized at room temperature and a hydrogen pressure of 0.3 MPa for 8 hours Allocation carried out in the same manner as in example 1.

Yield: 1.3 g (54%), Rf (A): 0,45;

1H-NMR (CDCl3, part./million): 9,65 (1H, s, CHO), 4,55 (1H, d, 1"'), 4,24 (1H, d, 1'), to 3.64 (3H, s, 3"'OMe), 3,51 (3H, s, 2"'OMe), of 2.51 (6H, s, NMe2), of 1.34 (3H, s, 12-CH3);

13C-NMR (CDCl3, frequent. /million): 212,30 (s, C-9), 202,36 (d, C-20), 170,27 (s, C-1), 103,29 (d, C-1'), 99,34 (d, C-1"'), 60,47 (q, 3"'OMe), 59,28 (s, C-12), 58,27 (q, 2"'OMe; d, C-13), 33,89 (t, C-10), 28,97 (t, C-11), 18,37 (q, C-22).

Example 5

The oxime 20-dimethylacetal 10,11-dihydro-12,13-amoxicilina (5)

3 g (3 mmole) of compound 1 was dissolved in 39 ml of pyridine, added to 1.25 g (18 mmol) of hydroxylaminopurine and stirred in a stream of nitrogen at room temperature in those who m pressure evaporated to one-third volume. The extraction is carried out with chloroform (2 servings 60 ml to pH 6, 2 portions of 60 ml to pH of 9.5). The combined extracts with pH of 9.5 was washed with a saturated solution of NaHCO3, dried (K2CO3) and evaporated to a dry residue.

Output: 1,83 g (61,3%), Rf (A): 0,45;

1H-NMR (DMSO, ppm million): 10,23 (1H, s, 9-NOH), disappears when mixed with D2O, 4,99 (1H, d, 1"), of 4.45 (1H, d, 1"'), 4,22 (1H, d, 1'), 3,49 (3H, s, 3"'OMe), of 3.45 (3H, s, 2"'OMe), 3,23 (3H, s, 20-OMe), 3,14 (3H, s, 20-OMe), 2,46 (6H, s, NMe2, 1,25 (3H, s, 12-CH3);

13C-NMR (CDCl3, part./million): 173,19 (s, C-1), 161,69 (s, C-9), 104,17 (d, C-1'), 102,06 (d, C-20), 100,64 (d, C-1"'), to 96.65 (d, C-1'), 62,30 (s, C-12), 61,69 (d, C-13), 61,43 (q, 3"'OMe), 59,09 (q, 2"'OMe), 16,32 (q, C-22).

Example 6

The oxime 20-dimethylacetal 10,11-dihydro-12,13-epoxidation (6)

2 g (2.4 mmole) of compound 3 was dissolved in 20 ml of methanol, added 0.64 g of Na2CO3and 0.84 g (12.3 mmole) of hydroxylaminopurine and stirred in a stream of nitrogen at its boiling point under reflux for 3 hours the Reaction solution is poured into 60 ml of water and the product emit extraction to a change in pH similar to that described in example 5.

Yield: 1.1 g (54%), Rf (A): 0,33;

1H-NMR (DMSO, ppm million): 10,22 (1H, s, 9-NOH), disappears when mixed with D2O, 4,43 (1H, d, 1"'), 4,19 (1H, d, 1'), 3,47 (3H, s, 3"'OMe), of 3.43 (3H, s, 2"'OMe), 3,21 (3H, s, C-9), 103,98 (d, C-1'), 102,05 (d, C-20), 100,51 (d, C-1"'), 62,27 (s, C-12), 61,73 (d, C-13), 61,42 (q, 3"'OMe), 59,09 (q, 2"'OMe), 16,30 (q, C-22).

Example 7

The oxime 10,11-dihydro-12,13-amoxicilina (7) and the oxime 10,11-dihydro-12,13-epoxidation (8)

2 g (2 mmole) of the compound (5) is dissolved in a mixture of 20 ml of acetonitrile with 20 ml of 0.2 H HCl and stirred at room temperature for 2 hours, the Reaction solution was diluted with 20 ml of water, alkalinized to pH 9 by adding NaOH, extracted with 2 portions of 30 ml of chloroform, dried (K2CO3) and evaporated to a dry residue. The crude product chromatografic on a column of silica gel.

Yield: 0.64 g (34%) of compound 7, Rf (B): 0,30;

1H-NMR (DMSO, ppm million): 10,23 (1H, s, 9-NOH), disappears when mixed with D2O 9,67 (1H, s, CHO), of 4.95 (1H, d, 1"), of 4.45 (1H, d, 1"'), is 4.21 (1H, d, 1'), 3,49 (3H, s, 3"'OMe), of 3.45 (3H, s, 2"'OMe), 2,47 (6H, s, NMe2), 1,25 (3H, s, 12-CH3);

13C-NMR (CDCl3, frequent. /million): 203,11 (d, C-20), 173,18 (s, C-1), 161,65 (s, C-9), 104,15 (d, C-1'), 100,62 (d, C-1"'), 96,63 (d, C-1"'), 62,30 (s, C-12), 61,76 (d, C-13), 61,42 (q, 3"'OMe), 59,25 (q, 2"'OMe), 16,46 (q, C-22);

and 0.35 g (23%) of compound 8, Rf (B): 0,22;

1H-NMR (DMSO, ppm million): of 10.21 (1H, s, 9-NOH), disappears when mixed with D2O, 9,68 (1H, s, CHO), 4,43 (1H, d, 1"'), 4,18 (1H, d, 1'), of 3.46 (3H, s, 3"'OMe), of 3.43 (3H, s, 2"'OMe), a 2.45 (6H, s, NMe2), to 1.22 (3H, s, 12-Snz);

13C-NMR (CDCl3, frequent. /million): 202,98 (d, C-20), 172,97 (s The oxime 10,11-dihydro-12,13-epoxidation (8)

1.3 g (1.5 mmole) of compound 6 was dissolved in a mixture of 13 ml of acetonitrile with 26 ml of 1% triperoxonane acid in water and stirred at room temperature for 2 hours the Product emit similar to that described in example 7.

Yield: 1 g (81%) of the compounds according to the spectral characteristics identical to those of compound 8 in example 7.

Example 9

The oxime 20-dimethylacetal 12,13-epoxidation (9) and 20-dimethylacetal 9-hydroxy-10,11-dihydro-12,13-epoxy-9,11- (epoxyamine)desmycosin (10)

2 g (2.4 mmole) 12,13-epoxidation-20-dimethylacetal dissolved in 16 ml of pyridine, add 1.0 g (14.4 mmole) of hydroxylaminopurine and the mixture is stirred in a stream of nitrogen at room temperature for 4 hours the reaction mixture was added 160 ml of water, alkalinized to pH 9 by adding 10% NaOH and extracted with 2 portions of 80 ml of chloroform. The combined extracts are dried and evaporated to a dry residue. 1,76 g crude product chromatografic on a column of silica gel in the solvent system A.

Output: 0,43 g (24%) of compound (9), Rf (A): 0,38;

1H-NMR (DMSO, ppm million): 10,42 (1H, s, 9-NOH), disappears when mixed with D2O, to 6.58 (1H, d, 11), to 6.43 (1H, d, 10), to 4.46 (1H, d, 1"'), to 4.23 (1H, d, 1'), 3,50 (3H, s, 3"'OMe), of 3.45 (3H, s, 2"'OMe), 3,23 (3H, s, 20-OMe), 3,14 (3H, s, 20-OMe), 2,47 (6H, s, NMe2
and 0,83 g (47%) of compound 10, Rf (A): 0,32;

2H-NMR (DMSO, frequent. /million): of 4.45 (1H, d, 1"'), 4,22 (1H, d, 1'), 3,49 (3H, s, 3"'OMe), of 3.45 (3H, s, 2"'OMe), 3,23 (3H, s, 20-OMe), 3,14 (3H, s, 20-OMe), 2,46 (6H, s, NMe2);

13C-NMR (CDCl3, part./million): 170,04 (s, C-1), 110,23 (s, C-9), 104,08 (d, C-1'), 102,51 (d, C-20), 100,24 (d, C-1"'), 63,37 (d, C-13), 61,44 (q, 3"'OMe), 60,67 (s, C-12), $ 59.13 USD (q, 2"'OMe), 54,34 (d, C-11), 15,24 (s, C-22).

1. Derivatives 12,13-amoxicilina formula I

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where R is Oh, R1represents Cho or CH(och3)2, R2denotes H or mikrosil and----- indicates a single bond; or where R denotes PONT, R1represents Cho or CH(och3)2, R2denotes H or mikrosil and---- denotes a single or double bond;

or the compound of formula II

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where R denotes H or mikrosil.

2. The compound of formula I on p. 1, representing 20 dimethylacetal 10,11-dihydro-12,13-amoxicilina.

3. The compound of formula I on p. 1, representing 10,11-dihydro-12,13-amoxiciloin.

4. The compound of formula I on p. 1, representing 20 dimethylacetal 4'-democaratic-10,11-dihydro-12,13-amoxicilina.

5. The compound of formula I under item 1, which represents a 4'-democaratic-Catala 10,11-dihydro-12,13-amoxicilina.

7. The compound of formula I on p. 1, representing the oxime 20-dimethylacetal 4'-democaratic-10,11-dihydro-12,13-amoxicilina.

8. The compound of formula I on p. 1, representing the oxime 10,11-dihydro-12,13-amoxicilina.

9. The compound of formula I on p. 1, representing the reaction of 4'-democaratic-10,11-dihydro-12,13-amoxicilina.

10. The compound of formula I on p. 1, representing the oxime 20-dimethylacetal 12,13-amoxicilina.

11. The compound of formula I on p. 1, representing the oxime 20-dimethylacetal 4'-democaratic-12,13-amoxicilina.

12. The compound of formula I on p. 1, representing the oxime 12,13-amoxicilina.

13. The compound of formula I on p. 1, representing the reaction of 4'-democaratic-12,13-amoxicilina.

14. The compound of formula II under item 1, representing 20 dimethylacetal 9-hydroxy-10,11-dihydro-12,13-epoxy-9,11-(epoxyamine)tylosin.

15. The compound of formula II under item 1, representing 20 dimethylacetal 4'-democaratic-9-hydroxy-10,11-dihydro-12,13-epoxy-9,11-(epoxyamine)tylosin.

16. The method of obtaining derivatives 12,13-amoxicilina formula I

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where R denotes O;

R1represents Cho or CH(och3)2
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where R1represents Cho or CH(och3)2;

R2denotes H or mikrosil;

R3denotes N(CH3)2or N-(och3)2provided that R2denotes H,

subjected to the hydrogenation reaction in an organic solvent, preferably in the lower C1-C3aliphatic alcohol, in the presence of 2 - 5% palladium on charcoal, under a hydrogen pressure of 0.2 - 0.5 MPa at room temperature for 5 to 8 hours

17. The method of obtaining derivatives 12,13-amoxicilina formula I

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where R has a value of PONT;

R1represents Cho or CH(och3)2;

R2denotes H or mikrosil;

line---- denotes a single or double bond,

and the compounds of formula II

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where R2denotes H or mikrosil,

characterized in that the compound of formula I, where R is Oh, R1denotes CH(och3)2, R2denotes H or mikrosil, and the line---- denotes a single bond, is subjected to reaction oxymorphine 3 to 6 equivalents of hydroxylamine hydrochloride in pyridine or a lower alcohol in the presence of a base such as pyridine or PA2COwith subsequent optional hydrolysis acetamino group; or the compound of formula III, where R1has the value of CH(och3)2, R2is set to N or mikrosil, R3has the value of N(CH3)2, is subjected to reaction oxymorphine described method, and the obtained compound of formula I, where R denotes PONT, R1denotes CH(och3)2, R2denotes H or mikrosil, line---- represents a double bond, and the compounds of formula II, where R2denotes H or mikrosil, divided by column chromatography on silica gel with subsequent optional hydrolysis acetamino group.

 

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