A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones

Autor:	Lan-Ying Qin, Kurt W. Saionz, Roland E. Dolle, Baldwin John J, Marc-Raleigh Brescia, Joan J. Zhang, James R. Wareing, Ian R. Henderson, Juerg Zimmermann, Axel Metzger, Pascal Rigollier, Hubert Gstach, Andrew G. Cole
Rok vydání:	2010
Předmět:	Organic Chemistry Biochemistry Combinatorial chemistry Chloride Acylation chemistry.chemical_compound chemistry Yield (chemistry) Drug Discovery medicine Amine gas treating Derivative (chemistry) Cysteine medicine.drug
Zdroj:	Tetrahedron Letters. 51:4486-4489
ISSN:	0040-4039
Popis:	A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones is described. The synthesis was developed on solid phase and was applied to provide a series of analogs in good yield. The key reactions are acylation of a cysteine derivative with 2,4-dichloropyrimidine-5-carbonyl chloride followed by cyclization to generate a 6-arylmethyl-7-carboxamido-2-chloro-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-one, which is further derivatized with an amine to give the desired 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-one.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::612c6229b945ede53f82e56c7f50e463 https://doi.org/10.1016/j.tetlet.2010.06.070 Zobrazit plný text záznamu Full Text from ScienceDirect