Effects of Various Bases on Acid-Catalyzed Amination of 2-Chloro-5-ethylpyrimidine: Synthesis of PPARpan Agonist GW693085
摘要:
A unique buffering effect of various bases, i-Pr2NEt and CaCO3 in particular, was observed for the acid-catalyzed chloro displacement of 2-chloro-5-ethylpyrimidine with a 2-methyl-2-phenylpropanamine. The use of the carefully chosen bases was essential for the progression of the chloro displacement as well as the stability of the product in the presence of HCl formed. Research work leading to an efficient synthesis of PPARpan agonist GW693085 is described, featuring highly selective sequential N- and O-alkylations.
(EN) The present invention features calcilytic compounds. 'Calcilytic compounds' refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.(FR) La présente invention concerne des 'composés calcilytiques', c'est-à-dire des composés pouvant inhiber l'activité du récepteur du calcium. On décrit également l'utilisation de ces composés pour inhiber l'activité dudit récepteur et/ou obtenir un effet bénéfique chez un patient, ainsi que des techniques que l'on peut utiliser pour obtenir d'autres composés calcilytiques.
Effects of Various Bases on Acid-Catalyzed Amination of 2-Chloro-5-ethylpyrimidine: Synthesis of PPARpan Agonist GW693085
作者:Bobby N. Glover、Lynda A. Jones、Byron, S. Johnson、Alan Millar、Martin H. Osterhout、Shiping Xie
DOI:10.1021/jo100562s
日期:2010.6.4
A unique buffering effect of various bases, i-Pr2NEt and CaCO3 in particular, was observed for the acid-catalyzed chloro displacement of 2-chloro-5-ethylpyrimidine with a 2-methyl-2-phenylpropanamine. The use of the carefully chosen bases was essential for the progression of the chloro displacement as well as the stability of the product in the presence of HCl formed. Research work leading to an efficient synthesis of PPARpan agonist GW693085 is described, featuring highly selective sequential N- and O-alkylations.
Die Synthese von 6,7-Dihydro-2<i>H</i>-pyrimido[6, 1-<i>a</i>]isochinolin-4(3<i>H</i>)-onen und analogen Verbindungen und deren Wirkung als Blutpättchenaggregationshemmer
作者:Frank Kienzle、Yves Bounameaux、Rudolf E. Minder、Reto Muggli
DOI:10.1002/hlca.19860690722
日期:1986.10.29
Synthesis of 6,7-Dihydro-2H-pyrimido[6,1-a]isoquinolin-4(3H)-ones and Analogous Compounds and their Activity as Blood-Platelet Inhibitors
6,7-二氢-2 H-嘧啶基[6,1 - a ]异喹啉-4(3 H)-ones及其类似化合物的合成及其作为血小板抑制剂的活性