Ist das S‐O? Die im Titel bezeichneten Molekülgerüste verfügen über eine hoch aktive und ausreichend differenzierte S‐O‐Bindung für die effiziente Synthese enantiomerenreiner Sulfinamide. Die beschriebene Methode ist praktisch und umweltverträglich und könnte als Grundlage für ein ökonomisches kommerzielles Verfahren zur Herstellung sperriger Sulfinamide dienen.
An efficient and practical synthesis of enantiomerically pure P-chiral dihydrobenzooxaphosphole (BOP) core 1 is developed that is amenable to large scale preparation of the related ligand series. The unique epimerization of the P-chiral center of the undesired (R,R)-diastereomeric phosphine oxide 19 through chlorination followed by crystallization makes this chemical resolution method achieve 65% yield of desired (R,S)-diastereomer 12.
Process development for a scalable and green synthesis of chiral tert-butanesulfinamide (TBSA) on a multikilogram scale is reported. The process is based on the identification of a chiral sulfinyl transfer agent, benzo [1,3]oxathiozin-2-one, that contains active and differentiated S−N and S−O bonds, allowing the synthesis to proceed under mild reaction conditions. This method is practical and overcomes the disadvantages of earlier methods deploying harsh reaction conditions and hazardous and toxic reagents.
Ist das S‐O? Die im Titel bezeichneten Molekülgerüste verfügen über eine hoch aktive und ausreichend differenzierte S‐O‐Bindung für die effiziente Synthese enantiomerenreiner Sulfinamide. Die beschriebene Methode ist praktisch und umweltverträglich und könnte als Grundlage für ein ökonomisches kommerzielles Verfahren zur Herstellung sperriger Sulfinamide dienen.
An efficient general methodology for the synthesis of 4-quinolinyl ethers is demonstrated via a highly reactive S N Ar reaction of 4-quinolinyl sulfones with a range of structurally diversified 1°, 2°, and 3°alcohols with a wide substrate scope and high yields. By adapting this methodology, a convergent synthesis of a complex target of HCV NS3/4a protease inhibitor BI 201420 was accomplished.
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