- A chiral oxazoline for catalytic enantioselective Nozaki-Hiyama-Kishi allylation and vinylation of aldehydes
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Asymmetric allylation and vinylation of aldehydes with allyl halides and vinyl halides have been achieved using the chromium(II)-oxazoline catalyst. The catalyst promotes the highly efficient enantioselective Nozaki–Hiyama-Kishi (NHK) allylation of aldehydes using allyl bromide, producing the corresponding homoallylic alcohols in good yields (up to 84%) and a high level of enantioselectivity (up to 98% ee). Meanwhile, the NHK vinylation of aldehydes produce desired allylic alcohols in satisfactory yields (up to 88%) and a high level of enantioselectivity (up to 97% ee). We developed a reliable and milder protocol for preparing chiral homoallylic and allylic alcohols.
- Chen, Chinpiao,Kumbhar, Sharad V.
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- In pursuit of natural product leads: Synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4- carboxylic acid (A-33853) and its analogues: Discovery of N-(2-benzoxazol-2- ylphenyl)benzamides as novel
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The first synthesis and biological evaluation of antibiotic 31 (A-33853) and its analogues are reported. Initial screening for inhibition of L. donovani, T. b. rhodesiense, T. cruzi, and P. falciparum cultures followed by determination of IC50
- Tipparaju, Suresh K.,Joyasawal, Sipak,Pieroni, Marco,Kaiser, Marcel,Brun, Reto,Kozikowski, Alan P.
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supporting information; experimental part
p. 7344 - 7347
(2009/12/07)
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- Diazepane derivatives or salts thereof
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To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan deriva
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- SUBSTITUTED BENZENE DERIVATIVES OR SALTS THEREOF
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There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2'-[(5-chloro-2-pyridyl)carbamoyl)-6-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2'-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4'-bromo-6'-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.
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- Benzimidazole compounds as bradykinin antagonists
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PCT No. PCT/JP95/01478 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 25, 1995 PCT Pub. No. WO96/04251 PCT Pub. Date Feb. 15, 1996This invention relates to a heterocyclic compound of the formula: wherein a group of the formula: is a group of the formula: etc., X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
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- A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a]pyridine moiety
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Recently we reported on overcoming the species difference of our first orally active non-peptide bradykinin (BK) B2 receptor antagonists, incorporating an 8-[[3-(N-acylglycyl-N-methylamino)-2,6-dichlorobenzyl]oxy]- 3-halo-2-methylimidazo[1,2-α]
- Abe, Yoshito,Kayakiri, Hiroshi,Satoh, Shigeki,Inoue, Takayuki,Sawada, Yuki,Inamura, Noriaki,Asano, Masayuki,Aramori, Ichiro,Hatori, Chie,Sawai, Hiroe,Oku, Teruo,Tanaka, Hirokazu
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p. 4062 - 4079
(2007/10/03)
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- Heterocyclic amido derivatives of substituted benzoic acids and therapeutic compositions which contain them as active principle
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Heterocyclic amido derivatives of substituted benzoic acids of general formula (I): in which:, R1 is H; 3-OCH3; 3-Cl; 4-Cl; 5-Cl; 3-CH3; 5-CH3; or 3-OH; -CH2-COOH; or -CH2-CO2-C
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