768394-93-0Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF DIPHENYL AZETIDINONE DERIVATIVES
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, (2008/06/13)
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
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Page/Page column 35-36, (2008/06/13)
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.
