- A steps Hua Tini chemical synthesis method (by machine translation)
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The present invention provides a convenient steps Hua Tini chemical synthesis method, using the synthesis method adopted in the process of preparing steps Hua Tini cheap raw materials, is easy to obtain, and saves the production cost, and the adoption of the synthesis method of the high yield of the product, the whole in the preparation process of mild reaction conditions, the atom economy is high. (by machine translation)
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Paragraph 0054; 0055; 0056
(2017/03/25)
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- Controlling the Substitution Pattern of Hexasubstituted Naphthalenes by Aryne/Siloxyfuran Diels–Alder Additions: Regio- and Stereocontrolled Synthesis of Arizonin C1 Analogs
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3,4-Dimethoxybenz-1-yne and 2-siloxylated furans without or with a bromine atom at C-3 undergo Diels–Alder reactions with orientational selectivity. Hydrolysis furnished a bromine-free or a bromine-containing naphthalene, respectively. Bromination of the former provided a regioisomer of the latter. Either of the two compounds was processed to give a variety of unnatural naphthoquinonopyrano-γ-lactones. This occurred by a succession of (1) Heck coupling, (2) asymmetric dihydroxylation, (3) oxa-Pictet–Spengler cyclization, and (4) oxidation. The fifteen monomeric naphthoquinonopyrano-γ-lactone structures that we prepared resemble the natural product (–)-arizonin C1 or its C-5 epimer. Accordingly, they represent hexasubstituted naphthalenes likewise. The sixteenth naphthoquinonopyrano-γ-lactone that we synthesized is a kind of dimer. Its moieties are bridged differently than those in naturally occurring naphthoquinonopyrano-γ-lactone dimers.
- Neumeyer, Markus,Kopp, Julia,Brückner, Reinhard
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p. 2883 - 2915
(2017/06/06)
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- NOVEL CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF
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The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Paragraph 0171
(2014/03/25)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS
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This invention provides compounds of formula (1) wherein X is C3-7 cycloalkyl, pyridinyl, pyrimidinyl or phenyl ring optionally substituted as described in claim 1, R1, R3 and R4 are chosen from the groups listed in claim 1. R2 is chosen from various unsaturated acyl groups listed in claim 1, with certain compounds being disclaimed. Use as tyrosine kinase inhibitors for the treatment of cancer and certain kidney diseases such as polycystic kidney disease.
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- Substituted 3-cyanoquinolines
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This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
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- Substituted quinazoline derivatives
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This invention provides compounds of formula 1 having the structure wherein: X, R1, R2, R3, R4, Z, X, and n are as defined hereinbefore in the specification, which are useful as antineoplastic agents and in the treatment of certain kidney diseases, such as polycystic kidney disease.
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- REGIOSELECTIVE SYNTHESIS OF α-ALKYLATED-β,γ-ENOATES BY REDUCTION-ALKYLATION WITH CUPRATES-ALKYL HALIDES OF γ-(BENZOTHIAZOLE-2-THIO)-α,β-ENOATES
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γ-(Benzothiazole-2-thio)-α,β-enoates 3-5 are reductively cleaved by lithium or magnesium cuprates to give enoate anions which are alkylated in situ leading to α-alkylated-β,γ-enoates.The high regioselectivity of the alkylation step is applied to the synthesis of esters of the monoterpenoid lavandulic acid 12.
- Calo, Vincenzo,Lopez, Luigi,Pesce, Giannangelo
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p. 203 - 205
(2007/10/02)
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