POTENTIAL BILE-ACID METABOLITES .5. 12-BETA-HYDROXY ACIDS BY STEREOSELECTIVE REDUCTION

POTENTIAL BILE-ACID METABOLITES .5. 12-BETA-HYDROXY ACIDS BY STEREOSELECTIVE REDUCTION
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DOI:
10.1080/00397918108065741
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发表时间:
1981-01-01
影响因子:
2.1
通讯作者:
CHANG, FC
CHANG, FC
中科院分区:
化学4区
文献类型:
--
作者:
CHANG, FC

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根据前人的研究,实用的路线2到12β-羟基胆酸是通过相应的酮酸的Raney镍催化氢化得到的,但该方法存在几个缺点:(1)要求的催化剂与底物的比例过高,(2)反应通常很慢,完全还原时间从6小时(12-羟基胆酸)到48小时(某些二羟基酮酸),(3)从催化剂上吸附的产物回收不完全,以及(4)由于反应时间长,可能会发生副反应,如最近报道的2,在Raney镍还原3-β,7-二羟基-12-氧胆酸甲酯(1)时,需要48小时才能完成,发生了C-3的部分反转。
According to previous research the practical route2to 12β-hydroxycholanic3acids was by Raney nickel catalytic hydrogenation of the corresponding keto acids, but the method suffers from several disadvantages: (1) the required ratio of catalyst to substrate is inordinately high, (2) the reaction is usually slow, with complete reduction time ranging from 6 hours (12-oxocholanic acid) to 48 hours (certain dihydroxy keto acids), (3) recovery from the adsorbed product from the catalyst is incomplete, and (4) with long reaction times side reactions can occur, as was recently reported2cthat during Raney nickel reduction of methyl 3β, 7α-dihydroxy-12-oxocholanate (1), requiring 48 hours for completion, partial inversion at C-3 took place.