发明名称 ERYTHROMYCINS AND PROCESS FOR THEIR PREPARATION
摘要 Poly:ketide(s) of formulae (I) or (II) and their salts are new. In (I): R1 = ~a-branched 3-8C alkyl, alkenyl, alkynyl, alkoxyalkyl or alkylthioalkyl, all optionally substituted by one or more hydroxy; 5-8C cycloalkylalkyl in which alkyl is 2-5C ~a-branched; 3-8C cycloalkyl or 5-8C cycloalkenyl (both optionally substituted by methyl, one or more OH, 1-4C alkyl or halo); 3-6 membered oxygen or sulphur-containing heterocycle, saturated or (partly) unsaturated and optionally substituted by one or more 1-4C alkyl or halo; R1 may also be phenyl, optionally substituted by one or more of 1-4C alkyl, alkoxy or alkylthio, halo, OH, trifluoromethyl or cyano; or the group (a): X = O, S or methylene; a, b, c and d = independently 0-2, totalling not over 5; R2 and R6 = H or OH; R3, R4, R5, R7, R9 and R12 are each H, Me or Et; R8 = H or a compound of formula (Ia); R10 = OH or a compound of formula (Ib); R11 = H; or R10= R11= O (sic). In (II): R1 = H, 1-8C alkyl, 2-8C alkenyl or alkynyl, 1-6C alkoxy or alkylthio-substituted alkyl, all alkyl, alkoxy, alkenyl and alkynyl are optionally substituted by one or more OH or halo; cycloalkyl, cycloalkenyl or heterocyclyl as in (I), or SR14; R14 = 1-8C alkyl, 2-8C alkenyl or alkynyl, 3-8C cycloalkyl, 5-8C cycloalkenyl, phenyl (optionally substituted by 1-4C alkyl or alkoxy, or halo), or heterocyclyl as above; other R groups are as in (i) provided that when R3, R4, R5, R7, R9, and R12 are all Me, then R1 is not H or Me. In (I) and (II) one or more CHOH or CHOR groups are replaced by keto. N.B. Formula (Ia) is described in the specification as desosamine; when R13 is H, (Ib) is described as mycarose and when R13 is CH3, (Ib) is described as cladinose.
申请公布号 HU9902905(A2) 申请公布日期 1999.12.28
申请号 HU19990002905 申请日期 1997.07.04
申请人 Biotica Technology Limited;PFIZER Inc. 发明人 CORTES, JESUS;LEADLAY, PETER FRANCIS;PACEY, MICHAEL STEPHEN;STAUNTON, JAMES
分类号 C07H17/08;C12N15/62;C12P19/62 主分类号 C07H17/08
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