PEREJRA Devid E. (US),ПЕРЕЙРА Дэвид Е. (US),PEREJRA Devid E.,ПЕРЕЙРА Дэвид Е.
申请号：
RU2012150753
公开号：
RU0002608390C2
申请日:
2011.05.20
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention described herein relates to methods of obtaining macrolide antibacterial agents. In particular, invention relates to methods for preparing macrolides and ketolides from erythromycin A. Method of producing a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R10 is hydrogen or acyl； X is H； Y is OR7； where R7 is cladinose, alkyl or arylalkyl, or acyl or C(O)NR8R9, where each R8 and R9 is independently selected from a group, consisting of hydrogen, hydroxy, alkyl, alkoxy, aryl, aryalkyl, dimethylaminoalkyl, acyl, sulphonyl, ureido and carbamoyl； or R8 and R9 together with nitrogen atom attached thereto form a heterocycle； or X and Y together with a carbon atom attached thereto form a carbonyl； V is C(O), C(=NR11), CH(NR12, R13) or N(R14)CH2； where N(R14) is bonded to C-10 carbon atom； where R11 is a hydroxy or alkoxy； each R12 and R13 is independently selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, aryl, aryalkyl, dimethylaminoalkyl, acyl, sulphonyl, ureido and carbamoyl； R14 is hydrogen, hydroxy, alkyl, alkoxy, aryl, arylalkyl, dimethylaminoalkyl, acyl, sulphonyl, ureido or carbamoyl； W denotes H, F, Cl, Br, I or OH； A is CH2, C(O), C(O)O, C(O)NH, S(O)2, S(O)2NH or C(O)NHS(O)2； B is (CH2)n, where n is an integer from 0 to 10； or unsaturated carbon chain, containing from 2 to 10 carbon atoms； and C is hydrogen, hydroxy, alkyl, alkoxy, aryl, arylalkyl, acyl, acyloxy, sulphonyl, ureido or carbamoyl； where alkyl independently in each case represents a C1-C30 alkyl； aryl in each case is independently selected from a group consisting of phenyl, optionally substituted amino group, naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, tetrazinyl, quinolinyl, quinazolinyl, quinoxalinyl, thienyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, benzisoxazolyl, benzisothiazolyl； acyl in
