- HYDRAZINE COMPOUND AS BLOOD COAGULATION FACTOR Xa INHIBITOR
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Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from a 3-9 membered carbon ring or its phenyl ring, and a 4-10 membered heterocyclic ring or its benzo ring; Y and Z are independently selected from 4-9 membered saturated heterocyclic rings respectively; RI-3 are independently selected from H, F, Cl, Br, I, CN, OH, SH,NH2, CHO, COOH respectively, or selected from C1-10 alkyls or heteroalkyls optionally substituted by R01, C3-10 alkyls ring hydrocarbon groups or heterocyclic hydrocarbon groups, C1-10 alkyls or heteroalkyls substituted by C3-10 ring hydrocarbon groups or heterocyclic hydrocarbon group. The compound can be used as an anticoagulant for treating and preventing thrombotic disorders, and can meet the real needs of selectivity and a potent inhibitor for coagulation Xa.
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Paragraph 0097
(2017/04/11)
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- Generation of 1-aryl-3-methoxycarbonylnitrilimines and their reaction with halogen-containing unsaturated compounds
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Thermal decomposition of 1-(4-methoxyphenyl)- and 1-(4-fluorophenyl) hepta(methoxycarbonyl)-3a,7a-dihydroindazoles at 135 C in the presence of allyl or propargyl halides leads to the elimination of hexamethyl benzenehexacarboxylate and the formation of the corresponding pyrazolines or pyrazoles as the products of 1,3-dipolar cycloaddition of 1-aryl-3- methoxycarbonylnitrilimines to the multiple bonds of the substrates used. In the case of vinyl halides, the products of the target reactions are either obtained in low yields or nonexistent, with a side conversions taking place instead. Thus, for example, in the case of 1,1-dichloro-4-methylpenta-1,3-diene, besides hexamethyl benzenehexacarboxylate, 3,5,5-trichloro-2-methylpent-4-en-2-ol and arylchlorohydrazones MeO2CC(Cl)=N-NHAr were unexpectedly isolated as the main products, as well.
- Tomilov,Platonov,Okonnishnikova,Novikov,Volchkov
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p. 1138 - 1147
(2013/07/26)
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- 1,3-Dipolar cycloaddition of nitrile imines with functionalized acetylenes: Regiocontrolled Sc(OTf)3-catalyzed synthesis of 4- and 5-substituted pyrazoles
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1,3-Dipolar cycloaddition of C-aryl-N-aryl- and C-carboxymethyl-N-aryl- nitrile imines with functionalized acetylenes have been studied. Regioisomeric mixtures have been obtained with the 5-substituted pyrazole as the major cycloadduct. Under scandium triflate catalysis a reversal in the regiochemistry was observed, especially in the case of C-carboxymethyl-N-aryl-nitrile imines. Georg Thieme Verlag Stuttgart.
- Bonini, Bianca Flavia,Franchini, Mauro Comes,Gentili, Denis,Locatelli, Erika,Ricci, Alfredo
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p. 2328 - 2332
(2010/01/16)
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- Dipolarophilic behaviour of (arylsulfonyl)allenes towards nitrilimines
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The dipolarophilic behaviour of 1-[2-(acetylamino)phenylsulfonyl]propa-1,2-diene 1 towards a series of nitrilimines is here described. Mechanistic possibilities for the formation of pyrazolic products 4-7 are discussed. The Royal Society of Chemistry 2000
- Broggini, Gianluigi,Molteni, Giorgio
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p. 1685 - 1689
(2007/10/03)
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- HETEROCYCLES FROM NITRILE IMINES. PART I. 1,2,3,4-TETRAHYDRO-1,2,4,5-TETRAZINES
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The interaction between ketohydrazones and nitrile imines provides a new and direct synthetic route to 1,2,3,4-tetrahydro-1,2,4,5-tetrazines.Elemental analysis and spectral data are consistent with the assigned tetrazine ring system.
- El-Abadelah, Mustafa M.,Hussein, Ahmad Q.,Kamal, Marwan R.,Al-Adhami, Khaled H.
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p. 917 - 924
(2007/10/02)
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