首页> 外国专利> Process for the stereoselective microbial reduction of 4 - (3,4-dichlorophenyl) - dihydro - 1 (2H) - naftalenona racmica in a mixture of CIS and trans tetraloles,Comprising contacting the compound with a micro organism or Enzyme System Reduction, incubate the mixture, and recovering the enantiomer (S) of the compound.

Process for the stereoselective microbial reduction of 4 - (3,4-dichlorophenyl) - dihydro - 1 (2H) - naftalenona racmica in a mixture of CIS and trans tetraloles,Comprising contacting the compound with a micro organism or Enzyme System Reduction, incubate the mixture, and recovering the enantiomer (S) of the compound.

机译:在CIS和反式四元醇的混合物中将4-(3,4-二氯苯基)-二氢-1(2H)-萘甲萘的立体选择性微生物还原的过程,包括使该化合物与微生物接触或通过酶系统还原进行孵育混合物,并回收化合物的对映异构体(S)。

摘要

The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: CHEM which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or "chiral tetralone." The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).
机译:本发明涉及对消旋四氢萘酮进行以下立体选择性微生物还原的方法:包括使式(I)化合物与微生物接触的酶,或能够完成包括衍生自所述微生物的酶和所述酶的辅因子,并在足以产生式(II)的(4R)四氢萘酚而基本上不反应的式(V)的(4S)四氢萘酮的条件下孵育所得混合物,或“手性四氢萘酮”。手性四氢萘酮可用于舍曲林的合成。该方法还任选地包括将式(V)的(4S)四氢萘酮与式(II)的(4R)四氢萘酚分离。可以将(4R)四氢萘酚再循环以制备式(I)的化合物,并重复进行本主题方法以得到更多的所需的式(V)四氢萘酮(4S)。

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