- METHOD OF PRODUCING OPTICALLY ACTIVE ALCOHOL
-
This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity at large scale production. Aromatic ketones represented by formula (I) [wherein, R1 are selected from hydrogen atom, halogen atom, lower alkyl group etc. R2 is -(CH2)n-R3 [wherein, n is 1 to 5 integer. R3 are selected from hydrogen atom, halogen atom, lower alkoxycarbonyl group etc. and formula (II) and (III). {wherein, R4 is selected from lower alkyl group (1 to 5 carbon atom) etc. R5 and R6 are the same or different and are selected from hydrogen atom, halogen atom, lower alkyl group etc.}]] are reduced by sodium borohydride, chlorotrimethylsilane and optically active 2-[bis(4-methoxyphenyl)hydroxymethyl]pyrrolidine represented by formula (IV) to give optically active alcohol represented by formula (V) stereoselectively. (wherein, R1 and R2 are as defined above.)
- -
-
Page/Page column 12; 13
(2008/12/08)
-
- PROCESS FOR THE PREPARATION OF DIPHENYL AZETIDINONE DERIVATIVES
-
The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, R1 and/or R2 as defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain -amino carboxamides or -amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby.
- -
-
-
- METHOD FOR PRODUCING DIPHENYL AZETIDINONE DERIVATIVES
-
The invention relates to a method for producing diphenyl azetidinone derivatives of general formula (I) or forms protected in the substituents X, R1 and/or R2, wherein the symbols, substituents, and indices have the following designations: X = H, OH; Rl = OH, OCH3; R2 = F, CH2CH3, CH2NHR4; R3 = H, F; R4 = H, CO-(CH2-)nCO-R5, CO-(CH2-)nNHR6; n = whole numbers from 4 to 16; R5 = OH, NH-CH2-[CH(OH)-]mCH2OH; R6 = H, CO-[CH(OH)-]mCH2OH; and m = whole numbers from 1 to 5. According to said method, novel compounds of general formula (II), wherein Y = H, H; H, OH; H, OAc; H, OSi(alkyl)o(aryl)p where o, p = 0, 1, 2 or 3 and o + p = 3; H, OTHP; H, OC(Aryl)3; H, OCH2OAlkyl; H, OCH(OAlkyl)CH3; H, OAlkyl; H, OCH2aryl; Oalkyl, Oalkyl; and cyclic ketone acetyl such as O-(CH2-)q-O where q = 2 or 3, are reacted with imines of general formula (III) wherein R7 = R1and O protective groups and R8 = e.g. R2.
- -
-
Page/Page column 56-58
(2008/06/13)
-