109431-87-0Relevant articles and documents
Enantiospecific Synthesis of the (4R)-1-Azabicycloheptane Ring System
Houghton, Peter G.,Humphrey, Guy R.,Kennedy, Derek J.,Roberts, D. Craig,Wright, Stanley H. B.
, p. 1421 - 1424 (1993)
An enantioselective synthesis of (4R)-1-azabicycloheptane derivatives is described commencing from readily available trans-4-hydroxy-L-proline which is converted into the key intermediate (3R)-N-(tert-butoxycarbonyl)-3-methylsulfonyloxypyrrolidine 4.Reaction of the sulfonate ester 4 with an enolate anion yields a mixtute of (3R)-pyrrolidineacetic esters 8 and 9 which are reduced to the corresponding alcohols 10 and 11.Conversion of the alcohols into the sulfonate esters 12 and 13 followed by deprotection of the pyrrolidine nitrogen leads to cyclisation yielding the (4R)-1-azabicycloheptane derivatives 14 and 15.
NOVEL OXADIAZOLES
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Page/Page column 96-97, (2020/05/15)
The present invention relates to novel compound of Formula I, wherein, R1, A1, A2, A3, A4, A5, L1, A, L2 and R2 are as defined in the detailed description. The present invention also relates to a combination or a composition comprising the compound of Formula I.
Enantioselective α-Benzylation of Acyclic Esters Using π-Extended Electrophiles
Schwarz, Kevin J.,Yang, Chao,Fyfe, James W. B.,Snaddon, Thomas N.
supporting information, p. 12102 - 12105 (2018/09/11)
The first asymmetric cooperative Lewis base/palladium catalyzed benzylic alkylation of acyclic esters is reported. This reaction proceeds via stereodefined C1-ammonium enolate nucleophiles. Critical to its success was the identification of benzylic phosphate electrophiles, which were uniquely reactive. Alkylated products were obtained with very high levels of enantioselectivity, and this method has been applied toward the synthesis of the thrombin inhibitor DX-9065a.
