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A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones |
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| Authors: | Lan-Ying Qin Andrew G. Cole Marc-Raleigh Brescia Joan J. Zhang James R. Wareing Juerg Zimmermann John J. Baldwin |
| Affiliation: | a Ligand Pharmaceuticals Inc., 3000 Eastpark Blvd., Cranbury, NJ 08512, USA† b Novartis Institutes for Biomedical Research, Basel, Switzerland c Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA d Novartis Institutes for Biomedical Research, Vienna, Austria |
| 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. |
| Keywords: | Dihydropyrimidothiazepinone Solid phase |
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