183859-36-1Relevant articles and documents
Chemoenzymatic approach to enantiopure piperidine-based β-amino esters in organic solvents
Liljeblad, Arto,Kavenius, Hanna-Maija,Taehtinen, Petri,Kanerva, Liisa T.
, p. 181 - 191 (2007/10/03)
This research concentrates on the enantioselectivities of lipase-catalysed reactions with methyl esters of 2-piperidylacetic acid and 3-piperidinecarboxylic acid derivatives. N-Acetylated 2-piperidylacetic acid methyl ester displayed good enantioselectivi
Enzymatic resolution of cyclic N-Boc protected β-aminoacids
Pousset, Cyrille,Callens, Roland,Haddad, Mansour,Larcheveque, Marc
, p. 3407 - 3412 (2007/10/03)
Methyl and ethyl esters of N-Boc homoproline, homopipecolic acid and 3-carboxymethyl-morpholine were kinetically resolved by hydrolysis catalysed by Burkholderia cepacia lipase to give the corresponding acids and residual esters in enantiomeric excesses better than 99% (E > 100).
Kowalski ester homologation. Application to the synthesis of β-amino esters
Gray, Diane,Concellon, Carmen,Gallagher, Timothy
, p. 4849 - 4851 (2007/10/03)
The Kowalski ester homologation protocol has been applied to a representative range of α-amino esters to provide β-amino esters with excellent levels of enantio- and diastereocontrol. A key feature of this chemistry is the nature of the N-protecting group that is employed.
Complex-induced proximity effects: The effect of varying directing-group orientation on carbamate-directed lithiation reactions
Bertini Gross,Beak
, p. 315 - 321 (2007/10/03)
A series of selected bicyclic carbamates in which the range of accessible angles and distances between the carbonyl group and the proton removed in an α-lithiation reaction are structurally defined have been investigated. Oxazolidinones 7-10 undergo stereoselective lithiation-substitution reactions to provide cis-18-27 and cis-31-35 as the major diastereomers. Two series of competition experiments show that the conformationally restricted carbamates 7, 10, 11, and 15 undergo lithiation via complexes more efficiently than Boc amines 4-6. These results along with semiempirical calculations suggest that a small dihedral angle and a calculated distance of 2.78 A between the carbamate carbonyl oxygen and the proton to be removed are favorable for a carbamate-directed lithiation. A series of tin-lithium exchange experiments on cis- and trans-18 and (S)-39 indicate that the configurational stability of a carbamate-stabilized organolithium species may be enhanced by restrictive geometry.
Antagonists of gonadotropin releasing hormone
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, (2008/06/13)
PCT No. PCT/US97/08428 Sec. 371 Date Nov. 12, 1998 Sec. 102(e) Date Nov. 12, 1998 PCT Filed May 16, 1997 PCT Pub. No. WO97/44037 PCT Pub. Date Nov. 27, 1997There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.
Antagonists of gonadotropin releasing hormone
-
, (2008/06/13)
PCT No. PCT/US97/08782 Sec. 371 Date Nov. 12, 1998 Sec. 102(e) Date Nov. 12, 1998 PCT Filed May 16, 1997 PCT Pub. No. WO97/44041 PCT Pub. Date Nov. 27, 1997There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.