Title of article :
A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones
Author/Authors :
Qin، نويسنده , , Lan-Ying and Cole، نويسنده , , Andrew G. and Metzger، نويسنده , , Axel and Brescia، نويسنده , , Marc-Raleigh and Saionz، نويسنده , , Kurt W. and Zhang، نويسنده , , Joan J. and Rigollier، نويسنده , , Pascal and Wareing، نويسنده , , James R. and Gstach، نويسنده , , Franz-Hubert and Zimmermann، نويسنده , , Juerg and Dolle، نويسنده , , Roland E. and Baldwin، نويسنده , , John J. and Henders، نويسنده ,
Abstract :
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.
