Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based Î³-secretase modulators.

Wu, Yong-Jin; Zhang, Yunhui; Toyn, Jeremy H; Macor, John E; Thompson, Lorin A

Wu, Yong-Jin; Zhang, Yunhui; Toyn, Jeremy H; Macor, John E; Thompson, Lorin A.

Afiliação

Wu YJ; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States. Electronic address: Yong-Jin.wu@bms.com.
Zhang Y; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States.
Toyn JH; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States.
Macor JE; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States.
Thompson LA; Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States.

Bioorg Med Chem Lett ; 26(6): 1554-1557, 2016 Mar 15.

Article em En | MEDLINE | ID: mdl-26898338

ABSTRACT

ABSTRACT

This Letter describes an efficient ring-closing metathesis approach to 2-chloro-4-amino-pyrimido[4,5-c]azepines and 2-chloro-4-amino-pyrimido[4,5-c]oxepines. These chlorides were applied to the synthesis of several potent Î³-secretase modulators (GSMs).

Assuntos

Secretases da Proteína Precursora do Amiloide/metabolismo; Azepinas/farmacologia; Oxepinas/farmacologia; Pirimidinas/farmacologia; Azepinas/síntese química; Azepinas/química; Relação Dose-Resposta a Droga; Humanos; Estrutura Molecular; Oxepinas/síntese química; Oxepinas/química; Pirimidinas/síntese química; Pirimidinas/química; Relação Estrutura-Atividade

Palavras-chave

2-Chloro-pyrimido[4,5-c]azepin-4-amine; 2-Chloro-pyrimido[4,5-c]oxepin-4-amine; Ring-closing metathesis (RCM); Î³-Secretase modulator (GSM)

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oxepinas / Pirimidinas / Azepinas / Secretases da Proteína Precursora do Amiloide Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article

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