50888-83-0Relevant academic research and scientific papers
Small organic molecule catalyzed enantioselective direct aldol reaction in water
Chimni, Swapandeep Singh,Mahajan, Dinesh
, p. 2108 - 2119 (2007/10/03)
Protonated pyrrolidine based small organic molecules have been designed and evaluated for the asymmetric direct aldol reaction in water. The designed organocatalysts are multifunctional in nature and exploit the combined effect of hydrogen bonding and hydrophobic interactions for enantioselective catalysis in water. As a result a unique direct asymmetric aldol reaction in water catalyzed by a small organic molecule having an amide linkage has been developed. The developed catalyst affords chiral β-hydroxyketones in good yields (93%) and enantioselectivities (upto 62%) in water.
Amino acids and peptides. XVI. Synthesis of N-terminal tetrapeptide analogs of fibrin α-chain and their inhibitory effects on fibrinogen/thrombin clotting
Kawasaki,Hirase,Miyano,Tsuji,Iwamoto
, p. 3253 - 3260 (2007/10/02)
N-Terminal tetrapeptide analogs of fibrin α-chain were synthesized by the solution method using a new active ester, the ester of the oxime of p-nitroacetophenone, and by the solid-phase method. Their inhibitory effects on fibrinogen/thrombin clotting were examined. Of the synthetic peptides, amide analogs of Gly-Pro-Arg-Pro exhibited a more potent inhibitory effect.
CONDENSED DIAZEPINONES, THEIR COMPOSITIONS AND METHODS OF USE AS PHARMACEUTICALS
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, (2008/06/13)
Disclosed are novel condensed diazepinones of formula I STR1 wherein B is a fused ring selected from STR2 X is--CH--or, when B is ortho-phenylene, X can also be nitrogen; A 1 is C 1-C. sub.2 alkylene; A 2 is C 1-C 2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3-or 4-position; R 1 is C 1-C 3 alkyl; R 2 is C. sub.1-C 7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C 3-C 7 cycloalkyl, optionally hydroxy substituted, or C 3-C 7 cycloalkylmethyl; or R 1 and R 2 can, together with the nitrogen therebetween, be a 4-to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH 3 ; R 3 is hydrogen, chlorine, or methyl; R 4 is hydrogen or C 1-C 4 alkyl, R 5 is hydrogen, chlorine or C 1-C 4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR 1 R 2--N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
