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Synthesis of a 6-CF3-Substituted 2-Amino-dihydro-1,3-thiazine ß-Secretase Inhibitor by N, N-Diethylaminosulfur Trifluoride-Mediated Chemoselective Cyclization.
J Org Chem ; 84(8): 4893-4897, 2019 04 19.
Article em En | MEDLINE | ID: mdl-30371078
The synthesis of a 6-CF3-substituted 2-amino-dihydro-1,3-thiazine via N, N-diethylaminosulfur trifluoride (DAST)-mediated cyclization of N-hydroxypropyl thiourea 6 is described. This reaction gave 6-CF3-1,3-thiazine 7 with high chemical yield and chemoselectivity, suppressing the common byproduct of oxazine 8. This new protocol enabled access to 6-CF3-substituted 1,3-thiazine ß-secretase inhibitor 2.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tiazinas / Dietilaminas / Inibidores Enzimáticos / Secretases da Proteína Precursora do Amiloide / Flúor Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tiazinas / Dietilaminas / Inibidores Enzimáticos / Secretases da Proteína Precursora do Amiloide / Flúor Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article