南方科技大学知识苑(SUSTech KC): 一种手性β-锗基-α-氨基酸及其合成方法

Title	一种手性β-锗基-α-氨基酸及其合成方法
Alternative Title	Chiral beta-germanium-alpha-amino acid and synthesis method thereof
Author	何川 ; 林伟栋
First Inventor	何川
Original applicant	南方科技大学
First applicant	南方科技大学
Address of First applicant	518055 广东省深圳市南山区桃源街道学苑大道1088号
Current applicant	南方科技大学
Address of Current applicant	518055 广东省深圳市南山区桃源街道学苑大道1088号 (广东,深圳,南山区)
First Current Applicant	南方科技大学
Address of First Current Applicant	518055 广东省深圳市南山区桃源街道学苑大道1088号 (广东,深圳,南山区)
Application Number	CN202210858597.8
Application Date	2022-07-20
Open (Notice) Number	CN115385951A
Date Available	2022-11-25
Status of Patent	实质审查
Legal Date	2022-12-13
Subtype	发明申请
SUSTech Authorship	First
Abstract	本发明属于不对称合成领域，公开了一种手性β‑锗基‑α‑氨基酸及其合成方法。其具有通式Ⅰ的结构或对映异构体、非对映异构体：其中，PG选自Phth、Cbz、Boc、Fmoc、Tos、PMB、Bn、Alloc；R1选自烷基、1‑金刚烷基、苯基、R4选自烷基、卤素、烷氧基、环烷基、苯基；R2、R3各自独立地选自以下结构之一：氢，苯基，苄基，萘基，烷基、烷氧基、卤素、三氟甲基、苯基、三甲基硅基、吗啉基取代的苯基，且R2、R3不同时为氢。本发明开发了一种铜催化的非天然β‑锗基α‑氨基酸的不对称合成方法，获得了各种手性β‑锗基‑α‑氨基酸衍生物，具有产率高、对映选择性好、底物适用范围广等优点；发明的化合物结构新颖，现有技术中未披露此类骨架的化合物。
Other Abstract	The invention belongs to the field of asymmetric synthesis, and discloses chiral beta-germanium-alpha-amino acid and a synthesis method thereof. The compound has a structure as shown in a general formula I or an enantiomer and a diastereomer, wherein PG is selected from Phth, Cbz, Boc, Fmoc, Tos, PMB, Bn and Alloc; r1 is selected from alkyl, 1-adamantyl and phenyl, and R4 is selected from alkyl, halogen, alkoxy, cycloalkyl and phenyl; r2 and R3 are independently selected from one of the following structures: hydrogen, phenyl, benzyl, naphthyl, alkyl, alkoxy, halogen, trifluoromethyl, phenyl, trimethylsilyl and morpholinyl substituted phenyl, and R2 and R3 are not hydrogen at the same time. According to the asymmetric synthesis method of the copper-catalyzed non-natural beta-germanium-based alpha-amino acid, various chiral beta-germanium-based alpha-amino acid derivatives are obtained, and the asymmetric synthesis method has the advantages of being high in yield, good in enantioselectivity, wide in substrate application range and the like; the compounds are novel in structure, and compounds with such skeletons are not disclosed in the prior art.
IPC Classification Number	C07F7/30
INPADOC Legal Status	（ENTRY INTO FORCE OF REQUEST FOR SUBSTANTIVE EXAMINATION）[2022-12-13][CN]
INPADOC Patent Family Count	1
Extended Patent Family Count	1
Priority date	2022-07-20
Patent Agent	曾敬
Agency	深圳市创富知识产权代理有限公司
URL	[Source Record]
Data Source	PatSnap
Document Type	Patent
Identifier	http://kc.sustech.edu.cn/handle/2SGJ60CL/534411
Department	Department of Chemistry
Recommended Citation GB/T 7714	何川,林伟栋. 一种手性β-锗基-α-氨基酸及其合成方法.

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