一种不对称有机膦催化高效合成光学活性多取代2，3-二氢苯并呋喃类化合物的方法

李鹏飞; 程玉宇; 方志强

李鹏飞

南方科技大学

南方科技大学

518055 广东省深圳市南山区西丽学苑大道1088号

南方科技大学

518055 广东省深圳市南山区西丽学苑大道1088号 (广东,深圳,南山区)

南方科技大学

518055 广东省深圳市南山区西丽学苑大道1088号 (广东,深圳,南山区)

CN201810695112.1

2018-06-29

CN108997368B

2020-02-21

2020-02-21

授权

2020-02-21

授权发明

第一

本发明属于有机合成方法领域，公开了一种不对称有机膦催化高效合成光学活性多取代2，3‑二氢苯并呋喃类化合物的方法，以手性膦化合物为催化剂，式A1化合物或式A2化合物和式B化合物反应，分别得到式C1化合物或式C2化合物：其中，R1为烷基，R2为烷基或苄基，R3为烷基，R4为氢、卤素或烷氧基，R5为氢、卤素或烷氧基。本发明的方法催化效果好，Morita‑Baylis‑Hillman碳酸酯与邻醌甲基化物反应，得到一系列光学活性的2，3‑二氢苯并呋喃，产率高，立体选择性好，催化效率高，操作简单，成本低廉，具有非常良好的工业化应用前景。

The invention belongs to the field of an organic synthesis method and discloses a method for efficiently synthesizing an optically active poly-substituted 2,3-dihydrobenzofuran compound through catalysis of asymmetric organic phosphine. A chiral phosphine compound serves as a catalyst, and a compound of a formula A1 or a compound of a formula A2 or a compound of a formula B perform reaction to obtain a compound of a formula C1 or a compound of a formula C2 separately (the formulas are as shown in the specification), wherein R1 is alkyl, R2 is alkyl or benzyl, R3 is alkyl, R4 is hydrogen, halogen or alkoxy and R5 is hydrogen, halogen or alkoxy. According to the method, the catalytic effect is good; Morita-Baylis-Hillman carbonic ester reacts with an o-quinone methyl compound to obtain a series of 2,3-dihydrobenzofuran with optical activity; and the method is high in yield, high in stereoselectivity, high in catalytic efficiency, simple to operate and low in cost, and has a very good industrialized application prospect.

C07B2200/07 ; C07D307/80 ; C07D493/04

C07D493/04 ; C07D307/80

（+PATENT GRANT）[2020-02-21][CN]

1

1

刘昌刚

深圳市深可信专利代理有限公司

PatSnap

李鹏飞,程玉宇,方志强. 一种不对称有机膦催化高效合成光学活性多取代2，3-二氢苯并呋喃类化合物的方法[P]. 2020-02-21.