- Synthesis process of ambroxol hydrochloride
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The invention relates to a synthesis process of ambroxol hydrochloride. The method comprises the following steps: carrying out bromination reaction on methyl anthranilate under the action of molecularbromine and hydrogen peroxide to generate a compound 3;
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Paragraph 0033-0038; 0057-0058
(2020/05/08)
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- 1-CYANO-PYRROLIDINE DERIVATIVES AS DUB INHIBITORS
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The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
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Paragraph 0901-0902
(2020/11/30)
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- A preparation method of bromhexine hydrochloride (by machine translation)
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The invention belongs to the field of organic synthesis, provides a bromhexine hydrochloride of the preparation method. The invention relates to 2 - aminobenzoic acid ester compound as a raw material, by the bromo reaction, reduction reaction, condensatio
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Paragraph 0063; 0101; 0103; 0104
(2019/04/10)
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- Cu-mediated selective bromination of aniline derivatives and preliminary mechanism study
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A simple and efficient bromination of aniline, aniline derivatives, and analogs have been developed. Forty three examples were given and the highest yield reached was 98%. Different substrates including substituted aniline, pyridin-amine, N-substituted aniline, N,N-disubstituted aniline, N-phenyl-amide, N-phenyl-sulfonamide, and nitrogen-containing heterocycles were all reactive and selectively generated desired bromo-products. The method can be applied to synthesize drug intermediate and quinoxaline derivatives.
- Zhao, Hong-Yi,Yang, Xue-Yan,Lei, Hao,Xin, Minhang,Zhang, San-Qi
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supporting information
p. 1406 - 1415
(2019/05/01)
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- Design, synthesis and optical response of pyridine-cored V-shaped stilbenoid dendrimers
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Design, synthesis and characterization of new series of first-generation V-shaped dendrimers bearing phenylenevinylene dendritic branches in periphery and pyridine as a core is described. A preliminary study of the optical properties of the resulting compounds was conducted by UV/vis and fluorescence spectroscopy.
- Jana, Debabrata,Ghorai, Binay K.
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scheme or table
p. 203 - 207
(2011/07/08)
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- Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists
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A 5,7-dichloro-3-phenyl-3-methyl-quinoline-2,4-dione (11a) has been identified in a random screen as a lead for 5-HT6 antagonist. During the lead optimization process, several analogs were synthesized and their biological activities were investigated. Within this series, several compounds display high binding affinity and selectivity for the 5-HT6 receptor. In particular, 3-(4-hydroxyphenyl)-3-methyl-quinoline-2,4-dione (12f) exhibits high affinity (Ki = 12.3 nM) for 5-HT6 receptor with good selectivity over other serotonin and dopamine (D1-D4) receptor subtypes. In a functional adenylyl cyclase stimulation assay, this compound exhibited considerable antagonistic activity (IC50 = 0.61 μM).
- Seong, Churl Min,Park, Woo Kyu,Park, Chul Min,Kong, Jae Yang,Park, No Sang
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p. 738 - 743
(2008/12/23)
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- Synthesis of dendritic stilbenoid compounds: Heck reactions for the periphery and the core
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A convergent synthetic strategy for stilbenoid dendrimers is described in which multifold Heck reactions have been used to construct both the peripheral and the core stilbene units. Solution optical properties of one of the dendrimers indicated some energy transfer having taken place from the periphery to the core.
- Sengupta, Saumitra,Sadhukhan, Subir Kumar,Singh, Rajkumar Sunil,Pal, Nilasish
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p. 1117 - 1121
(2007/10/03)
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- Mild and regioselective oxidative bromination of anilines using potassium bromide and sodium perborate
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The selective monobromination of various deactivated anilines using potassium bromide and sodium perborate as oxidant has been achieved. The use of ammonium molybdate as catalyst accelerates the rate of reaction but is not essential to obtain good yields and high selectivities. (C) 2000 Elsevier Science Ltd.
- Roche, Didier,Prasad, Kapa,Repic, Oljan,Blacklock, Thomas J.
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p. 2083 - 2085
(2007/10/03)
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- Chiroptical Detection During Liquid Chromatography, Part 5: On-Line Measurement of Circular Dichroism Spectra Δε(λ) During Stops of Chromatographic Flow
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A procedure is described which serves to measure circular dichrograms Δε(λ) on line during stops of flow in liquid chromatography.Since the concentration of substrate in the spectrometer cell during the stop is not known, the differential absorption coeff
- Brandl, Gert,Kastner, Fritz,Fritsch, Rainer,Zinner, Herbert,Mannschreck, Albrecht
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p. 1059 - 1070
(2007/10/02)
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- Process for the selective reduction of the 4-halogen in 2,4-dihaloanilines
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Substituted 2-haloanilines are prepared from the correspondingly substituted 2,4-dichloro- or 2,4-dibromoanilines by selectively reducing a chloro or bromo substituent para to a protected amino group in the presence of the same halogen as an ortho substit
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