Practical chemoenzymatic synthesis of a 3-pyridylethanolamino β 3 adrenergic receptor agonist
…, J Leazer, R Farr, M Robbins, K Emerson, DJ Mathre…
文献索引：Chung, John Y. L.; Ho, Guo-Jie; Chartrain, Michel; Roberge, Chris; Zhao, Dalian; Leazer, John; Farr, Roger; Robbins, Micheal; Emerson, Kateeta; Mathre, David J.; McNamara, James M.; Hughes, David L.; Grabowski, Edward J. J.; Reider, Paul J. Tetrahedron Letters, 1999 , vol. 40, # 37 p. 6739 - 6743
A chemoenzymatic synthesis of β3 agonist 1 suitable for large scale preparation is described. The key chiral 3-pyridylethanolamine intermediate (R)-7 was prepared via an improved Neber rearrangement and a yeast-mediated asymmetric reduction. The tetrazolone fragment of the molecule was constructed via a dipolar cycloaddition between 1- (cyclopentyl)-3-propylazide and p-chlorosulfonyl phenylisocyanate. Sulfonamide coupling ...
