Preparation of taxoid compounds (I) comprises reacting an optionally protected taxene compound (II) with a molecular sieve base in sulfolane, condensing with a side chain, and removing protecting groups. Preparation of taxoid compounds of formula (I) comprises reacting an optionally protected taxene compound of formula (II) with a basic molecular sieve in sulfolane to cyclize the 7 beta -trifluoromethyl sulfonyloxy group, condensing with a side chain, and removing protecting groups. [Image] Ar : aryl; R : H, acetyl, alkoxyacetyl or alkyl; R 1benzoyl or R 2-O-CO; R 21-8C alkyl; R' : a protecting group when R in (I) is H, or R. An independent claim is also included for the preparation of intermediate compounds of formula (III) which comprises reacting (II) with a molecular sieve base in sulfolane. [Image] ACTIVITY : None given. MECHANISM OF ACTION : None given.
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机译:紫杉烷化合物(I)的制备包括使任选保护的紫杉烯化合物(II)与环丁砜中的分子筛碱反应,与侧链缩合,并除去保护基。式(I)的紫杉类化合物的制备包括使任选被保护的式(II)的紫杉类化合物与碱性分子筛在环丁砜中反应,以环化7β-三氟甲基磺酰氧基,与侧链缩合,并除去保护基。 [图像] Ar:芳基; R:H,乙酰基,烷氧基乙酰基或烷基; R 1苯甲酰基或R 2 -O-CO; R 21-8C烷基; R':当(I)中的R为H或R时的保护基。还包括用于制备式(III)的中间体化合物的独立权利要求,所述中间体化合物包括使(II)与分子筛碱在环丁砜中反应。 [图像]活动:未给出。作用机理:未给出。
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