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