191152-27-9Relevant articles and documents
A convergent synthesis approach towards CGP60536B, a non-peptide orally potent renin inhibitor, via an enantiomerically pure ketolactone intermediate
Rueger,Stutz,Goschke,Spindler,Maibaum
, p. 10085 - 10089 (2007/10/03)
We report a convergent synthesis of the potent orally active non-peptide renin inhibitor CGP60536B. The key reaction employs the coupling of the enantiopure Grignard species derived from chloride 13 with the diastereomerically pure γlactone 9b. The stereoselective reduction of the resulting ketone 14b has been thoroughly investigated. (C) 2000 Elsevier Science Ltd.
Synthesis of (4S)-hydroxymethyl-(2R)-(2-propyl)-butyrolactone: A quest for a practical route to an important hydroxyethylene isostere chiron
Hanessian, Stephen,Abad-Grillo, Teresa,McNaughton-Smith, Grant
, p. 6281 - 6294 (2007/10/03)
Several approaches for the stereocontrolled introduction of a 2-propyl group into (4S)-hydroxymethyl-1,4-butyrolactone via cholate chemistry were investigated. A practical synthesis of the (2R)- and (2S)-isomers was developed.