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
› Institutsangaben

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).
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Publikationsverlauf

Received: 10. Mai 2018

Accepted after revision: 12. Juni 2018

Publikationsdatum:
31. Juli 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