Abstract
Tetrahydroisoquinolines (THIQs) with a C1-aryl-substituted groups are common in many natural and synthetic compounds of biological importance. Currently, their enantioselective synthesis are majorly reliant on chemical catalysis. Enzymatic synthesis using imine reductase is very attractive due to the cost-effectiveness, high catalytic efficiency and enantioselectivity. However the steric-hindrance of the 1-aryl substituents make this conversion very challenging, and current successful examples are most-ly restricted to the simple alkyl-THIQs. In this report, through extensive evaluation of a large collection of IREDs (including 88 novel enzymes), we successfully identified a panel of steric-hindrance tolerated IREDs. These enzymes are able to convert me-ta-, para-substituted chloro-, methyl-, and methoxyl-benzyl DHIQs (dihydroisoquinolines) into corresponding R- or S- THIQs with very high enantioselectivity and conversion. Among them, the two most hindrance-tolerated enzymes (with different ste-reo-specif...
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