Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 86, Issue 18, Pages 12783-12801Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c01413
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- Enamine Ltd
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This study elaborates a general practical approach to hetero(aromatic) and aliphatic P(O)Me-2-substituted derivatives, where the key synthetic step was a [Pd]-mediated C-P coupling of (hetero)aryl bromides/iodides with HP(O)Me-2. The P(O)Me-2 substituent was found to significantly increase solubility and decrease lipophilicity of organic compounds, and this tactic was successfully used to enhance the solubility of the antihypertensive drug prazosin without altering its biological profile.
A general practical approach to hetero(aromatic) and aliphatic P(O)Me-2-substituted derivatives is elaborated. The key synthetic step was a [Pd]-mediated C-P coupling of (hetero)aryl bromides/iodides with HP(O)Me-2. The P(O)Me-2 substituent was shown to dramatically increase solubility and decrease Iipophilicity 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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