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Asymmetric urea compounds and method of manufacturing the asymmetric compound by asymmetric conjugate addition reaction using this as a catalyst
Asymmetric urea compounds and method of manufacturing the asymmetric compound by asymmetric conjugate addition reaction using this as a catalyst
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机译:不对称脲化合物和使用不对称脲化合物作为催化剂通过不对称共轭加成反应制备不对称化合物的方法
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摘要
The present invention relates to a production method of asymmetric compound (IV) which includes conjugately adding nucleophilic reagent (III) to compound (II) in the presence of asymmetric urea compound (I). The present invention provides a non-metallic asymmetric catalyst capable of realizing a highly stereoselective asymmetric conjugate addition reaction in a high yield, and an advantageous production method of an asymmetric compound by an asymmetric conjugate addition reaction using the asymmetric catalyst. wherein X is an oxygen atom or a sulfur atom; C*, C** and C*** are asymmetric carbons; R 1 , R 2 , R 4 , R 5 , R 8 , R 9 and R 10 are each a lower alkyl group optionally having substituent(s) and the like, or R 4 and R 5 and the like in combination optionally form a homocyclic ring optionally having substituent(s) and the like; R 3 is an aryl group optionally having substituent(s) and the like; R 6 and R 7 are each a hydrogen atom and the like; Nu is -CR 16 (COR 17 ) (COR 18 ) wherein R 16 , R 17 and R 18 are each a lower alkyl group optionally having substituent(s) and the like, and the like; and EWG is an electron withdrawing group.
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机译:本发明涉及不对称化合物(IV)的制备方法,该方法包括在不对称脲化合物(I)存在下,将亲核试剂(III)共轭添加到化合物(II)中。本发明提供了能够以高收率实现高立体选择性的不对称共轭加成反应的非金属不对称催化剂,以及使用不对称催化剂通过不对称共轭加成反应制备不对称化合物的有利方法。其中X是氧原子或硫原子; C *,C **和C ***为不对称碳; R 1,R 2,R 4,R 5,R 8,R 9和R 10各自为任选具有取代基等的低级烷基,或者R 4和R 5等组合组合任选地形成a。任选具有取代基等的同环; R 3为任选具有取代基等的芳基。 R 6和R 7各自为氢原子等。 Nu为-CR 16(COR 17)(COR 18),其中R 16,R 17和R 18分别为任选具有取代基等的低级烷基等。 EWG是吸电子基团。
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