177839-89-3Relevant academic research and scientific papers
Practical asymmetric synthesis of Sitagliptin phosphate monohydrate
Gao, Haoling,Yu, Jiangang,Ge, Chengsheng,Jiang, Qun
, (2018)
Optically pure sitagliptin phosphate monohydrate is efficiently and practically synthesized through a chiral hemiacetal as the key intermediate in 54% overall yield starting from (E)-4-(2,4,5-trifluorophenyl)but-2-enal and N-boc-protected hydroxylamine. The chiral hemiacetal fragment is constructed by a tandem aza-Michael/hemiacetal reaction catalyzed by an organocatalyst and the influence of acidity of Br?nsted acid on tandem aza-Michael/hemiacetal reaction is researched in detail.
Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
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Page/Page column 62-63, (2008/12/07)
Provided herein are Heterocyclic Compounds having the following structure: wherein R1, R2, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.
Inhibitors of farnesyl protein transferase
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, (2008/06/13)
Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.
Preparation of 'carba' dipeptides bearing a basic side-chain at the C-terminus: Synthesis of enantiopure Boc-D-Phe-Ψ[CH2CH2]-L-Arg(NO2)-OH and Boc-D-Phe-Ψ[CH2CH2]-D-Arg(NO2)OH
Kende, Andrew S.,Dong, Han-Qing,Mazur, Adam W.,Ebetino, Frank H.
, p. 6015 - 6018 (2007/10/03)
A new approach to synthesize 'carba' Ψ[CH2CH2] dipeptides, e.g. Boc-D-Phe-Ψ[CH2CH2]-L-Arg(NO2)-OH and Boc-D-Phe-Ψ[CH2CH2]-D-Arg(NO2)-OH, is described.
A novel approach to homochiral β-amino acids 1
Seki, Masahiko,Matsumoto, Kazuo
, p. 3165 - 3168 (2007/10/03)
An efficient synthesis of γ-aryl or alkyl substituted β-amino acids starting from N-Cbz-L-homoserine lactone via the formation of α-amino aryl, alkenyl or alkynyl ketones with the original α-carbon chirality retained as such is described. Copyright
