CAS: 1134-47-0; 4-Amino-3-(4-Chlorophenyl)Butanoic Acid

相似化合物

186320-20-7 78131-31-4 66514-99-6

上下游产品

4-(4-chlorophenyl)pyrrolidin-2-one ethyl 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(4-chlorophenyl)butanoate ethyl 3-(4-chlorophenyl)-3-hydroxybutanoate (E)-3-(4-chlorophenyl)but-2-enoic acidn-chloro°Ctane 4-Amino-3-(4-chloro-phenyl)-butyric acid °Ctyl ester; hydr°Chloride 4-(4-chlorophenyl)pyrrolidin-2-one 3-(4-chlorophenyl)-4-pyrrol-1-ylbutyric acid

Baclofen Hydrochloride置于ammonium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 2.0H,以41%的收率获得巴氯芬
参考文献:外消旋巴氯芬的结构表征和 Hirshfeld 表面分析
标题:外消旋巴氯芬的结构表征和 Hirshfeld 表面分析
摘要:摘要 巴氯芬 (R,S) [4-氨基-3-(4-氯苯基)丁酸] (C10H12Clno2,Mr = 213.66) 的晶体结构已通过单晶 X 射线衍射分析确定.标题化合物在正交空间群 Pbca (No. 61) 中结晶,A = 9.2704(5),B = 7.0397(4),C = 30.4015(15) A,V = 1984.0(2) A3 和 Z = 8.分子以两性离子形式存在,相对于 Cα Cβ 键采用 Gauche 构象,并通过强 Nh⋯o 氢键和 C Cl⋯π 相互作用保持在交联链排列中.通过 Hirshfeld 表面分析标题化合物的静电分子势以及分子间相互作用.还报告了 Ft-Ir 光谱.Dta,Tg 和 Dtg 结果表明巴氯芬在高达 205 oc 时是稳定的.
Doi:10.1016/j.Molstruc.2016.06.041

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-11807883-B2
优先权日:2020-11-03
标 题:Polypeptide tag, highly soluble recombinant nitrilase and application thereof in synthesis of pharmaceutical chemicals
发明人：XUE YAPING; XIE DONG; XIONG NENG; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a polypeptide tag and its application in the synthesis of pharmaceutical chemicals, the recombinant nitrilase was obtained by connecting a polypeptide tag to the N-terminus of the amino acid sequence of the nitrilase; wherein amino acids at both ends of the polypeptide tag are uncharged glycine G, and the rest are a random combination of any one or more of glycine G, histidine H, glutamic acid E, aspartic acid D, lysine K and arginine R; The activity of the recombinant nitrilase in the preparation of 1-cyanocyclohexyl acetic acid is up to 3034.7 U/g dcw, the polypeptide tag significantly improves the soluble expression of nitrilase, and the whole cell catalyst hydrolyzes 1M substrate with the same concentration 30 minutes faster than the mother enzyme. The method provided by the present invention can also be used for the biocatalytic reaction of other pharmaceutical intermediates as the substrate catalyzed by the nitrilase, improving the activity of the whole cell catalyst in reaction, and also improving the solubility of other types of nitrilases and the activity of the corresponding whole cell catalysts.

专利号:WO-2015183067-A1
优先权日:2014-05-30
标题 :Synthesis of analogues of y-amino acids and resulting products
发明人：FERNÃ?NDEZ ZERTUCHE MARIO; TOVAR GUDIÑO ERIKA; TRUJILLO FERRARA JOSÉ GUADALUPE; GUEVARA SALAZAR JUAN ALBERTO
权利人:UNIV AUTÓNOMA DEL ESTADO DE MORELOS
摘要:The invention relates to a compound of formula (see formula), suitable for use as drugs in the treatment of chronic neurodegenerative disorders of the Huntington's disease, Parkinson's disease and epilepsy type, inter alia . The invention relates to novel methods for the synthesis of said analogues and the pharmaceutically acceptable solvates and salts thereof.

专利号:US-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.

专利号:EP-3599246-A1
优先权日:2018-07-25
标题 :Means and methods for synthesizing precursors of y-aminobutyric acid (gaba) analogs
发明人：POELARENDS GERRIT JAN; BIEWENGA LIEUWE; VAN DER MEER JAN-YTZEN; PODDAR HARSHWARDHAN; THANGAVELU SARAVANAN
权利人:UNIV GRONINGEN
摘要:The invention relates to the fields of drug development and biocatalysis, more specifically to a biocatalytic route for asymmetric synthesis of precursors of y-aminobutyric acid (GABA) analogs. Provided is an isolated mutant 4-oxalocrototonate tautomerase (4-OT) enzyme comprising the following mutations (i) leucine at position 8 substituted with a tyrosine (L8Y) or a phenylalanine (L8F); (ii) methionine at position 45 substituted with a tyrosine (M45Y); and (iii) phenylalanine at position 50 substituted with an alanine (F50A), wherein the positions are numbered according to the amino acid sequence of 4-OT ofPseudomonas putida.Also provided is a method for the synthesis of a precursor for the pharmaceutically relevant enantiomer of a GABA analog, comprising (i) providing a y-nitroaldehyde using the 4-OT mutant enzyme, followed by (ii) subjecting the thus obtained y-nitroaldehyde to an enzymatic oxidation reaction catalyzed by an aldehyde dehydrogenase (EC 1.2.1.3).

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.