An efficient and flexible route to novel triazolopiperazine scaffolds

被引：1

作者：

Lorthioir, Olivier ^{[1
]}

Greenwood, Ryan D. ^{[1
]}

Lister, Andrew ^{[1
]}

Tucker, Michael J. ^{[1
]}

机构：

[1] AstraZeneca, Med Chem, Oncol R&D, Cambridge CB4 0WG, England

来源：

TETRAHEDRON LETTERS | 2020年 / 61卷 / 50期

关键词：

Fused rings; Semi-saturated heterocycles; Triazole synthesis; Spirocycles; Oxetanes; ASYMMETRIC ALPHA-AMINATION; MEDICINAL CHEMISTS; DRUG DISCOVERY; OXETANES; SPIROCYCLES; ALCOHOLS; DESIGN;

D O I：

10.1016/j.tetlet.2020.152600

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In this work we describe the preparation of novel fused, spirocyclic and chiral triazolopiperazines. We have developed a practical, rapid and robust synthetic route to these scaffolds that allows control of regio- and stereochemistry. This method utilises mild conditions and uses widely available and diverse amino acids and amidines as starting materials. These complex unprecedented 5,6,7,8-tetrahydro-[1-2,4]triazolo[1,5-alpha]pyrazines represent attractive building blocks for drug discovery. (C) 2020 Elsevier Ltd. All rights reserved.

引用

页数：4

共 50 条

[1] A Flexible Route to Indole Scaffolds - Formal Synthesis of (±)-Mersicarpine
Pfaffenbach, Magnus
Gaich, Tanja
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2015, 2015 (16) : 3427 - 3429
[2] A novel and efficient route to Zafirlukast
Srinivas, K
Srinivasan, N
Krishna, MR
Reddy, CR
Arunagiri, M
Lalitha, R
Reddy, KSR
Reddy, BS
Reddy, GM
Reddy, PP
Kumar, MK
Reddy, MS
ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2004, 8 (06) : 952 - 954
[3] A novel and efficient route for the preparation of atorvastatin
Gao, Jian
Guo, Yang Hui
Wang, Ya Ping
Wang, Xiang Jing
Xiang, Wen Sheng
CHINESE CHEMICAL LETTERS, 2011, 22 (10) : 1159 - 1162
[4] A NOVEL EFFICIENT ROUTE TO HEXAHYDRODIBENZOFURAN DERIVATIVES
BERRIER, C
JOUANNETAUD, MP
JACQUESY, JC
KIGABO, F
TETRAHEDRON, 1991, 47 (33) : 6681 - 6688
[5] A short and efficient route to novel trishomocubanones
Singh, V
Jagadish, B
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1997, 36 (10): : 905 - 906
[6] A NOVEL AND EFFICIENT ROUTE TO PROSTANOID INTERMEDIATES
LEVIN, JI
TETRAHEDRON LETTERS, 1989, 30 (01) : 13 - 14
[7] A novel and efficient route for the preparation of atorvastatin
Jian Gao~a
Chinese Chemical Letters, 2011, 22 (10) : 1159 - 1162
[8] A novel and efficient route for synthesis of Taladegib
Guo, Mingliang
Hong, Kwon Ho
Lv, Yongfeng
Ding, Yu
Li, Congcong
Xu, Hua
Qi, Wenxiu
Chen, Junqing
Ji, Min
Cai, Jin
JOURNAL OF CHEMICAL RESEARCH, 2017, (02) : 112 - 115
[9] A novel route in bone tissue engineering: Magnetic biomimetic scaffolds
Bock, N.
Riminucci, A.
Dionigi, C.
Russo, A.
Tampieri, A.
Landi, E.
Goranov, V. A.
Marcacci, M.
Dediu, V.
ACTA BIOMATERIALIA, 2010, 6 (03) : 786 - 796
[10] Organic sol-gel chemistry as a flexible synthetic route to tissue engineering scaffolds
Borgaonkar, Poonam
Sharma, Sachin
Chen, Ming
Bhowmick, Sankha
Schmidt, Daniel F.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 234

← 1 2 3 4 5 →