Stereocontrolled synthesis of C2-symmetric and pseudo-C2-symmetric diamino alcohols and diols for use in HIV protease inhibitors

…, EM Doherty, SM Hannick, LM Codavoci…

Index: Kempf, Dale J.; Sowin, Thomas J.; Doherty, Elizabeth M.; Hannick, Steven M.; Codavoci, LynnMarie; et al. Journal of Organic Chemistry, 1992 , vol. 57, # 21 p. 5692 - 5700

Full Text: HTML

Citation Number: 91

Abstract

Method G. Coupling with BOP. To a stirred solution of the amino acid eater component (1- 01) in CHzClz (10 mL) were added BOP reagent (1.1 mmol), and diprotected N-(o- aminoalkylenelamino acids (1.1 mmol), DIEA (3 mmol) at room temperature. After 15 min the pH was checked for basicity (in casea where the pH was lower than pH= 9, more DIEA was added) and the reaction mixture left for 1 h at room temperature. The solvent was ...