Synthesis of New MeO-BIPHEP-type Chiral Diphosphines by an Improved Way

In this paper, a series of new optically active MeO-BIPHEP-type ligands, （S）-6,6＇-dimethoxy-2,2＇-bis（dip-alkoxyphenyl-phosphine）-l,l＇-biphenyl [（S）-5b-（S）-5e] were prepared and characterized. Starting from the commercially available triethyl phosphorite and m-bromoanisole, an optically active （S）-6,6＇-dimethoxybiphenyl- 2,2＇-diyl-bis（phosphonic acid diester） was prepared by an improved way and converted to the corresponding dichlorides, which was used as a key intermediate to react with p-alkoxybenzenemagnesium bromide or p-alkoxyphenyl lithium to directly give the enantiomerically pure diphosphines 5.

A Facile Synthesis of Enantiomerically Pure （R）-6-Arylbinols

This work reported a convenient method for the preparation of enantiomerically pure 6-aryl-2,2＇-dihydroxy-1, l＇- binaphthyl derivatives starting from the commercially available （R）-2,2＇-hydroxy-l, l＇-binaphthyl [（R）-I] via bromi- nation, hydrolysis and Suzuki cross coupling reaction. This novel synthetie method was characterized with high re- gioselectivity, simple operation, mild reaction conditions, and excellent yield （up to 73%）. On the other hand, we synthesized the target unknown compounds, which were confirmed by IR, 1H NMR, 13C NMR, MS and elementary analysis.

1,1′-联二萘酚的合成及其在不对称合成中的应用

1 ,1′-联二萘酚是具有 C2 -对称轴的手性原料 ,已广泛用于合成手性医药、农药、香料及食品添加剂中。较为详细地概述了 1 ,1′-联二萘酚的合成进展 。

手性桃潜蛾性信息素的新合成路线

桃潜蛾(peach leafminer moth;Lyonetiaclerkella,L.)属鳞翅目潜蛾科,在日本和我国辽东半岛等各地果园中危害极大。

Catalytic asymmetric Catellani-type reaction: A powerful tool for axial chirality construction

This highlight summarizes a recent development of a catalytic enantioselective Catellani-type reaction for the synthesis of axially chiral biaryls.The chirality induction is solely governed by chiral norbornene ligand in the Pd mediated ortho C–H functionalization and ipso cross-coupling transformation.The preparative power of the methodology is demonstrated as a powerful manifold for the divergent synthesis of structurally diverse axially chiral biaryls and chiral fluorenols.

阿伐他汀手性中间体合成研究进展

综述了近年来阿伐他汀手性中间体的合成研究进展,从手性池反应、不对称合成、外消旋体拆分三个方面介绍了阿伐他汀手性中间体合成的工艺路线和研究水平,对其工业化前景进行了展望。

(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇的合成工艺研究

目的对(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇合成工艺进行研究。方法以3-戊酮为起始原料,经Mannich反应、手性拆分、Grignard反应等步骤合成(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇,并对化学拆分进行工艺优化。结果合成(2S,3R)-1-二甲氨基-3-(3-甲氧基苯基)-2-甲基戊-3-醇,总收率为30.6%。结论工艺改进后提高了目标产物的收率,同时也减少了原料的浪费。