Synlett 2018; 29(14): 1867-1870
DOI: 10.1055/s-0037-1609906
letter
© Georg Thieme Verlag Stuttgart · New York

Highly Efficient Coupling of Unstable Bicyclic Pyrimidines and Pyrazoles under Basic Conditions, and its Application to the Synthesis of Pharmaceutical Compounds

Takashi Goi*
a   Research Unit/Immunology & Inflammation, Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation, 1000, Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan   Email: goi.takashi@mk.mt-pharma.co.jp
b   Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka, 560-0043, Japan
,
Koichi Fukase
b   Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka, 560-0043, Japan
› Author Affiliations
This research was supported by Mitsubishi Tanabe Pharma Corporation, JSPS KAKENHI Grant Number 15H05836 (KF) in Middle Molecular Strategy, and JSPS KAKENHI Grant Number 16H01885 (KF).
Further Information

Publication History

Received: 10 May 2018

Accepted after revision: 12 June 2018

Publication Date:
31 July 2018 (online)


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Abstract

The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd2(dba)3, t BuXPhos, and K3PO4.

Supporting Information