公开(公告)号：US5183749A

公开(公告)日：1993-02-02

申请号：US496183

申请日：1990-03-20

申请人： Gerado Ramos ,  Oreste Ghisalba ,  Hans-Peter Schar ,  Bruno Frei ,  Peter Maienfisch ,  Anthony C. O'Sullivan

发明人： Gerado Ramos ,  Oreste Ghisalba ,  Hans-Peter Schar ,  Bruno Frei ,  Peter Maienfisch ,  Anthony C. O'Sullivan

IPC分类号： A01N49/00 ,  C07H19/01 ,  C12P17/18

CPC分类号： C07H19/01 ,  A01N49/00 ,  C12P17/181 ,  C12R1/525 ,  C12R1/685 ,  Y10S435/822 ,  Y10S435/886 ,  Y10S435/911 ,  Y10S435/917

摘要： The present invention relates to a one-step microbial process for the preparation of 13.beta.-hydroxy- or 14,15-epoxy-milbemycins of the following formulae I and II ##STR1## in which R.sub.1 and R.sub.1 ' represent methyl, ethyl, isopropyl or sec.-butyl or represent the group ##STR2## in which X represents methyl, ethyl or isopropyl, and A and A' represent the group ##STR3## in which R.sub.2 represents hydrogen, --C(O)-CH.sub.2 O-C(O)-CH.sub.2 CH.sub.2 -COOH or --C(O)-CH.sub.2 CH.sub.2 -COOH, or mixtures of compounds of the formulae I and II, which process comprises bringing a milbemycin of the formula III ##STR4## dissolved in a liquid phase, in which R.sub.3 represents R.sub.1 or R.sub.1 ' and R.sub.4 represents A or A', and R.sub.1, R.sub.1 ', A and A' have the meanings given for formulae I and II, into contact with a microorganism that is capable of 13.beta.-hydroxylation or 14,15-epoxidation or of both reactions, or into contact with active constituents thereof. The microorganism or its active constituents may be either in free form or immobilized form.

摘要翻译： 本发明涉及一种用于制备下式I和II的13β-羟基或14,15-环氧 - 米尔倍霉素的一步微生物方法。其中R1 并且R 1'表示甲基，乙基，异丙基或仲丁基，或表示其中X表示甲基，乙基或异丙基的基团，A和A'表示其中R 2表示氢的基团，-C （O）-CH 2 O-C（O）-CH 2 CH 2 -COOH或-C（O）-CH 2 CH 2 -COOH，或式I和II化合物的混合物，该方法包括使式III的米尔倍霉素 III）溶解在液相中，其中R3表示R1或R1'，R4表示A或A'，R1，R1'，A和A'具有式I和II给出的含义，与微生物接触， 能够进行13β-羟基化或14,15-环氧化或两种反应，或与其活性成分接触。 微生物或其活性成分可以是游离形式或固定化形式。