专利号:WO-9221675-A1 优先权日:1991-06-03 标题:Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:EP-0643710-A1 优先权日:1991-06-03 标 题 :Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:US-5322942-A 优先权日:1991-06-03 标题 :Synthesis of optically active lactones from L-aspartic acid and intermediates thereof 发明人:RAPOPORT HENRY; DENER JEFFREY M; ZHANG LIN-HAU 权利人:UNIV CALIFORNIA 摘要:Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R 2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R 4 is H or C 1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C 1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R 4 is H, and Ar is 1-methylimidazol-5-yl.
参考文献:10.1107/s2053229614013163 摘要:Benali-Cherif R, Takouachet R, Bendeif el-E, Benali-Cherif N. A comparative study of two polymorphs of L-aspartic acid hydrochloride. Acta Crystallogr C Struct Chem. 2014 Jul;70(Pt 7):689–92. doi: 10.1107/s2053229614013163.