Production of N-substituted derivatives of 1-desoxy-nojirimycin
申请人:Bayer Aktiengesellschaft
公开号:US04266025A1
公开(公告)日:1981-05-05
The invention relates to a process for the production of compounds of the formula ##STR1## in which R is hydrogen or optionally substituted alkyl, alkenyl, aralkyl or aryl, by microbiological transformation of ##STR2## follow by catalytic hydrogenation. The compounds obtained are useful for the treatment of diabetes, hyperlipoproteinaemia and adiposity which comprises aerobically cultivates, in the presence of an assimilable source of carbon nitrogen, at a temperature of 20.degree. to 45.degree. C. and pH between 2 and 10 and in the presence of an effective amount of a compound of the formula ##STR3## in which R has the above-given meaning and, R.sub.1 denotes an optionally substituted benzyl radical or an optionally substituted .beta.-alkenyl group, an aerobic microorganism or an extract of aerobic microorganism capable, in a nutrient medium containing a compound of the formula (X), or accumulating an amount of a compound of the formula ##STR4## in which R and R.sub.1 have the above-mentioned meanings and subjecting the resulting compound of the general formula XI to catalytic hydrogenation.
Herstellung von N-substituierten Derivaten des 1-Desoxy-nojirimycins
申请人:BAYER AG
公开号:EP0012278A2
公开(公告)日:1980-06-25
Gegebenenfalls N-substituierte 1-Desoxynojirimycin-Verbindungen werden erhalten, indem man N-geschützte 1-Amino-1-desoxy-D-glucitole der Formel
worin R Wasserstoff, gegebenenfalls substituiertes Alkyl, Aralkyl oder Aryl und R1 gegebenenfalls substituiertes Benzyl oder ß-Alkenyl bedeuten, mit aeroben Mikroorganismen zu entsprechenden N-geschützten 6-Amino-6-desoxy-L-sorbose-Verbindungen der Formel
oxidiert und diese Verbindungen katalytisch hydriert.
通过使 N 保护的 1-氨基-1-脱氧-D-葡萄糖醇(式中 R 为氢,任选取代的烷基、芳基或芳基,R1 为任选取代的苄基或ß-烯基)与好氧微生物反应,可获得任选 N 取代的 1-脱氧野尻霉素化合物。
其中 R 是氢、任选取代的烷基、芳烷基或芳基,R1 是任选取代的苄基或 ß-烯基)与好氧微生物反应,得到相应的 N-保护的式 6-氨基-6-脱氧-L-山梨糖化合物。
并对这些化合物进行催化氢化。