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PROCESS FOR THE MANUFACTURING OF INTERMEDIATE PRODUCTS FOR THE SYNTHESIS OF GLUCOSE-6-PHOSPHATASE INHIBITORS AND NEW INTERMEDIATE PRODUCTS
PROCESS FOR THE MANUFACTURING OF INTERMEDIATE PRODUCTS FOR THE SYNTHESIS OF GLUCOSE-6-PHOSPHATASE INHIBITORS AND NEW INTERMEDIATE PRODUCTS
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机译:合成葡萄糖-6-磷酸酶抑制剂和新的中间产物的中间产物的生产过程
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摘要
The preparation of arylcyclopropylmethoxy-cyclohexanecarboxylic acid derivs. of formula (I) comprises a) base-catalysed hydrolysis of the lactone ring of a 1,2-O-cyclohexylidene-3,5-lactonyl-cyclohexane-1,2-diol of formula (II) to the alcohol of formula (III); treatment of (III) with acid chloride in the presence of base to give the ester of formula (IV); treatment of (IV) with carbene to give a mixt. of diastereoisomers (VA) and (VB) (the configuration at the C atoms marked with an asterisk being 2S,1R (VA) or 2R,1S (VB)). (VA) predominates and is sepd. from the mixt. by crystallisation prior to conversion into (I) by alkaline hydrolyses. R = F, Cl or Me. R1 = 1-10C alkyl or benzyl; R2 = 1-10C alkyl, phenyl or naphthyl. Compounds (I), (III), (IV) and (VA) are new.
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机译:制备芳基环丙基甲氧基-环己烷羧酸的衍生物。式(I)的化合物包括:a)将式(II)的1,2-O-环己叉基3,5-内酯基-环己烷-1,2-二醇的内酯环碱催化水解为式(II)的醇。 III);在碱存在下用酰氯处理(Ⅲ),得到式(Ⅳ)的酯;用卡宾处理(IV)得到混合物。非对映异构体(VA)和(VB)(在C原子上标有星号的构型为2S,1R(VA)或2R,1S(VB))。 (VA)占主导地位,并且是Sepd。从混音。在通过碱水解转化为(I)之前,通过结晶进行结晶。 R = F,Cl或Me。 R1 = 1-10C烷基或苄基; R 2 = 1-10C烷基,苯基或萘基。化合物(I),(III),(IV)和(VA)是新的。
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