CAS: 2909-38-8; 3-Chlorophenylisocyanate

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3-氯苯甲酸置于盐酸,硫酸,一水合肼,Sodium Nitrite体系中,用 甲醇,二氯甲烷,水,1,2-二氯乙烷 用作溶剂,化学反应 23.0H,反应生成间氯苯异氰酸酯
参考文献:新型脲基苯甲酰胺衍生物作为强效聚(adp-核糖)聚合酶-1(parp-1)抑制剂的设计,合成,生物学评价和分子对接研究
标题:新型脲基苯甲酰胺衍生物作为强效聚(adp-核糖)聚合酶-1(parp-1)抑制剂的设计,合成,生物学评价和分子对接研究
摘要:Poly(Adp-Ribose) Polymerase-1 (Parp-1) 是负责修复 Dna 单链断裂的 Dna 修复酶的关键成员之一.Parp-1的抑制已被证明是一种通过靶向dna修复途径选择性杀死肿瘤细胞的有前景的策略.在此,基于基于结构的药物设计策略,设计合成了一系列新型脲基苯甲酰胺衍生物.评价了对hct116,Mda-Mb-231,Hela,A579和a375等五种人类癌细胞系的抗癌活性,并总结了初步的构效关系.其中,化合物23F和27F对 Hct116 细胞具有有效的抗增殖作用,Ic 50值分别为 7.87 μm 和 8.93 μm.此外,两种化合物均表现出优异的 Parp-1 抑制活性,Ic 50值分别为 5.17 Nm 和 6.06 Nm.机理研究表明,23F和27F能有效抑制hct116细胞的集落形成和细胞迁移.此外,23F和27F可导致细胞周期停滞在g2/m期,并通过
Doi:10.1016/j.Ejmech.2022.114790

专利信息

专利号:US-4267070-A
优先权日:1979-10-30
标题:Catalyst for the synthesis of aromatic monoisocyanates
发明人：NEFEDOV BORIS K; MANOV-JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L
权利人:NEFEDOV BORIS K; MANOV JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L
摘要:A catalyst for the synthesis of aromatic monoisocyanates comprising 1.64 to 16.6% by weight of palladium chloride, 0.16 to 47.6% by weight of an oxide of a metal of Group VB of the periodic system, 1.5 to 81.8% by weight of an oxide of a metal of Group VI B of the periodic system, 1.64 to 89.8% by weight of pyridine or an alkylsubstituted pyridine. n The use of the catalyst according to the invention in the synthesis of aromatic monoisocyanates makes it possible to obtain a high degree of conversion of the starting compound of up to 100%, a high yield of the desired product of up to 97%, and increased productivity of the catalyst of up to 40 g of the desired product per g of PdCl 2 per hour.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-4341898-A
优先权日:1981-05-18
标题:Synthesis of isocyanates from nitroalkanes
发明人：MILLIGAN BARTON; PINSCHMIDT JR ROBERT K
权利人:AIR PROD & CHEM
摘要:A process for the preparation of aromatic isocyanates from nitroalkanes. A nitromethyl aromatic compound of the general formula: wherein R and R1 represent hydrogen, halogen, a C1-C5 alkyl radical, a C1-C4 alkoxy radical, nitro, isocyanato, an alkoxycarbonylamino, or nitromethyl radical, with R and R1 being the same or different, is heated in the presence of an effective amount of a Lewis acid or Bronsted acid substance to effect a dehydrogenation-isomerization reaction to yield an aromatic isocyanate of the general formula: The product of the reaction may be recovered as the aromatic isocyanate or the alcohol adduct, a carbamate.

专利号:US-9879050-B2
优先权日:2013-08-30
标 题 :Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase
发明人：LEE RICHARD E; ZHAO YING; GRIFFITH ELIZABETH; ZHENG ZHONG; SINGH AMAN P
权利人:ST JUDE CHILDREN'S RES HOSPITAL
摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9833457-B2
优先权日:2008-01-25
标题:Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
发明人：MJALLI ADNAN M M; GADDAM BAPU; POLISETTI DHARMA RAO; KOSTURA MATTHEW J; GUZEL MUSTAFA
权利人:VTV THERAPEUTICS LLC
摘要:The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to psoriatic arthritis.