- Preparation method of formaldehyde-substituted aza-condensed ring compound
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The invention provides a preparation method of a formaldehyde-substituted aza-condensed ring compound, comprising the following steps: by using an aza-condensed ring lactam compound as a starting material, carrying out halogenation reaction, methylation reaction and methyl oxidation reaction to obtain the formaldehyde-substituted aza-condensed ring compound. According to the preparation method ofthe formaldehyde-substituted aza-condensed ring compound, the whole synthesis route is good in step repeatability, mild in operation condition and high in safety, and large-scale production and industrial popularization are facilitated; post-treatment energy consumption is low, a large amount of toxic wastewater is not generated, no pollution is caused to the environment, the production safety level and the production cost are reduced, application of green and environment-friendly industrial production is facilitated, and wide application prospects are achieved.
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Paragraph 0125-0127
(2020/06/02)
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- The synthesis of azaperylene-9,10-dicarboximides
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The syntheses of two azaperylene 9,10-dicarboximides are presented. 1-Aza- and 1,6-diazaperylene 9,10-dicarboximides containing a 2,6-diisopropylphenyl substituent at the N-imide position were synthesized in two steps starting from naphthalene and isoquin
- Andrew, Trisha L.,Vanveller, Brett,Swager, Timothy M.
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supporting information; experimental part
p. 3045 - 3048
(2011/02/25)
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- Process for Preparing 1-Halo-2,7-Naphthyridinyl Derivatives
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A process for preparing 1-halo-2,7-naphthyridinyl derivatives is described (I), wherein X is Cl or Br; which process comprises the following steps: (i) reaction of a 3-cyano-4-methylpyridine derivative of formula (A): with a compound of formula (II), in the presence of an N,N-dimethylformamide diC1-6alkylacetal; to give an enamine derivative of formula (III), (ii) cyclisation of the enamine of formula (III), to obtain the compound of formula (IV), (iii) reaction of the compound of formula (IV) with a halogenating agent, to obtain a compound of formula (I).
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Page/Page column 8
(2009/09/08)
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- PHENYLALANINE ENAMIDE DERIVATIVES
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Phenylalanine enamide derivatives of formula (1) are described, wherein R1is a -CH(CH3)2, -(CH2)2CH3; -CH2C(CH3)3, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH2OH, -CH2CH2OCH2CH2OCH3, formula (A) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of α4 integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.
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- PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES
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A process for the preparation of a class of phenylalanine enamide derivatives is described formula (1) wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).
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- 2-SUBSTITUTED 1,2-BENZISOTHIAZOL-3(2H)-ONE 1,1-DIOXIDE USEFUL AS AN ANXIOLYTIC AGENT
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There is disclosed the compound 2-[4-[4-(2,7-naphthyridin-1-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3(2 H)-one 1,1-dioxide, and the method of producing said compound, and the pharmaceutically acceptable salts thereof, and the use of said compound as an anxiolytic agent having a low liability for extrapyramidal side effects.
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