Phosphine Oxides (-POMe2) for Medicinal Chemistry: Synthesis, Properties, and Applications.
J Org Chem
; 86(18): 12783-12801, 2021 09 17.
Article
em En
| MEDLINE
| ID: mdl-34468144
ABSTRACT
A general practical approach to hetero(aromatic) and aliphatic P(O)Me2-substituted derivatives is elaborated. The key synthetic step was a [Pd]-mediated C-P coupling of (hetero)aryl bromides/iodides with HP(O)Me2. The P(O)Me2 substituent was shown to dramatically increase solubility and decrease lipophilicity of organic compounds. This tactic was used to improve the solubility of the antihypertensive drug prazosin without affecting its biological profile.
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01-internacional
Base de dados:
MEDLINE
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Óxidos
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Idioma:
En
Revista:
J Org Chem
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Ucrânia