- Practical synthesis of a renin inhibitor via a diastereoselective dieckmann cyclization
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A scalable synthesis of a potent renin inhibitor (1) is described. The absolute stereochemistry is set via an unprecedented diastereoselective Dieckmann cyclization directed by a remote chiral protecting group. This transformation enables preparation of chiral 1,3-[3.3.1]-diazabicyclononenes by desymmetrization of alkyl-esters, with selectivities ranging from 4 to 17:1.
- Gauvreau, Danny,Hughes, Greg J.,Lau, Stephen Y. W.,McKay, Daniel J.,O'Shea, Paul D.,Sidler, Rick R.,Yu, Bing,Davies, Ian W.
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supporting information; experimental part
p. 5146 - 5149
(2011/02/23)
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- A PROCESS FOR PREPARING DIAZABICYCLO[3.3.1] NONANE COMPOUNDS
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The invention is a process for preparing a diazabicyclo compound of formula (I) process for preparing a diazabicyclo compound of formula (I):where X is selected from the group consisting of hydrogen, C1-C6 alkoxycarbonyl, and carbobenzyloxy; R6 is selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, and benzyl; and R9, R 10, and R11 are independently selected from the group consisting of hydrogen, halogen, and C1-C6 alkyl. wherein the process involves cyclizing I-I, formula (II).
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Page/Page column 22
(2008/12/07)
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