| 摘要 |
Enzymatic acylation process for alcohols is claimed. The process comprises: (a) reacting an ester of formula (I) with an alcohol of formula (II) or (IV) in the presence of lipase (L), and isolating the optically pure alcohol, and opt. the other enantiomers, from the ester obtd. (L) is derived from porcine liver or pancreas, or microorganisms such as Candida, Penicillium, Mucor, Rhizopus, Aspergillus and Pseudomonas. R1 = H, 1-18C alkyl (opt. substd. by halo), phenyl or 1-3C alkoxy-(1-4C)-alkyl; R2 = H or E or Z Me; R3 = Me, Et, Pr, i-Pr or n-Bu; R4 = 1-18C alkyl or 3-10C cycloalkyl (both opt. halogenated); R5 = 1-5C epoxyalkyl (with the epoxy gp. beta - to the OH gp.), 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl or 3-8C cycloalkenyl (these 4 opt. substd. by COOH, halo, NO2, CN, 1-4C alkoxy or Ph), or aryl or heteroaryl (both opt. substd. by 1-4C alkyl, 1-4C alkoxy, halo, NO2, CN or NA); or R4+R5 = a gp. of formula (a) or (b) (sic), or the alkenylene (a) or (b) forms a keto gp.; Ph = phenyl (opt. substd. by halo, NO2, CN or 1-4C alkoxy); NA = protected amino; n = 1-3; R6,R7 = H, 2-4C alkenyl or 1-4C alkyl; or R6+R7 = anellated phenyl or naphthyl (both opt. substd. by 1-4C alkyl, 1-4C alkoxy, NO2, CN or halo); R8 = H or alkyl; R9 = XR10, R10 = alkyl, aralkyl, aryl, benzyl or naphthylmethyl; X = bond or O.
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