Author/Authors :
Chen، نويسنده , , Jinshan and Rong، نويسنده , , Frank and Shan، نويسنده , , Bo and Chen، نويسنده , , Yuanwei and Li، نويسنده , , Yingfu and Yu، نويسنده , , Hua and Chen، نويسنده , , Li and Kuang، نويسنده , , Tongtao and Li، نويسنده , , Shai and Chen، نويسنده , , Youpei and Du، نويسنده , , Jing and Ai، نويسنده , , Chaowu and Li، نويسنده , , Jian and Li، نويسنده , , Xiaoyong and Shi، نويسنده , , Changqing and Jiang، نويسنده , , Zhilong and Long، نويسنده ,
Abstract :
We report novel syntheses of 12-membered macrocyclic templates and a library of 4000 macrocyclic analogs. The key macrocyclization step was performed at up to 100 g scale without resorting to syringe pumps, flow reactors or large volumes of solvent. An interesting observation of considerably different permeability properties was made on diastereomeric analogs due to differences in intramolecular hydrogen bond interactions.
Keywords :
Macrocyclization , 12-Membered ring , Lactam cyclization , Intra-molecular hydrogen bond , Permeability
