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1,1'-bis-(diphenylphosphino)ferr°Cene diamminedichloropalladium(II) {1,1'-bis(diphenylphosphino)ferr°Cene} palladium dibromide dichloromethane 1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-phenylbenzene]-1-benzenesulfonamideN1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-phenylbenzene]-1-benzenesulfonamide 1-(phenylsulfonyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline 1-[2-chloro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-N1-methyl-1-benzenesulfonamideN1-[2-chloro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-N1-methyl-1-benzenesulfonamide methyl 3-[(2R)-2-({(tert-butoxycarbonyl)[(2R)-2-{[tert-butyl(dimethyl)silyl]oxy}-2-(3-pyridinyl)ethyl]amino}methyl)-3,4-dihydro-2H-chromen-6-yl]benzoate 合成工艺路线路线简述
- 合成目标产物 [1,1'-Bis(Diphenylphosphino)Ferrocene]Dichloropalladium(Ii) 主要起始原料 1,1'-Bis(Diphenylphosphino)Ferrocene And Palladium, Bis(Acetonitrile)Dichloro-, (Sp-4-2)-
- (文献来源)合成步骤主要原料 1,1'-Bis(Diphenylphosphino)Ferrocene 和 Palladium, Bis(Acetonitrile)Dichloro-, (Sp-4-2)-
羟乙酸甲酯 以 四氢呋喃,Petroleum Ether作为反应溶剂,获得 (1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride
参考文献:Antibacterial Piperidinyl Substituted 3,4-Dihydro-1H-[1,8]Naphthyridinones
标题:Antibacterial Piperidinyl Substituted 3,4-Dihydro-1H-[1,8]Naphthyridinones
摘要:本发明涉及一种公式(I)的新化合物,其抑制fab1酶的活性,因此在治疗细菌感染方面非常有用.此外,本发明还涉及包含这些化合物的药物组合物以及制备这些化合物的化学过程.
专利信息
专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-2004018598-A1
优先权日:2000-05-30
标题 :Bio-intermediates for use in the chemical synthesis of polyketides
发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C
摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:WO-2024183094-A1
优先权日:2023-03-07
标 题 :Use of ligand catalyst in synthesis of indole alkaloids
发明人:YAN PUCHA; Cheng Houan; ZHOU BO; HUA YUNYU; SUN ZEBIN; FU XINGFENG; LI YUANQIANG
权利人:ZHEJIANG JIUZHOU PHARM CO LTD
摘要:The present invention provides use of a ligand catalyst in the synthesis of indole alkaloids. The ligand catalyst is formula (1). A method for the catalytic synthesis of the indole alkaloids comprises the following steps: sequentially adding reactants, a metal catalyst, a ligand catalyst, an oxidizing agent, and an additive into a reaction container, adding an organic solvent, carrying out the reaction, and carrying out separation and purification to obtain an indole derivative. The chemical reaction formula of the indole derivative is as follows: formula (2), wherein R1 is selected from one of hydrogen, alkyl, alkoxy, and aryl, R2 is selected from one of trifluoromethanesulfonyl, p-toluenesulfonyl, hydrogen, and alkyl, R3 is selected from one of alkyl, alkoxy, aryl, and heteroaryl, and R4 is selected from one of hydrogen, alkyl, alkoxy, aryl, and heteroaryl. The present invention solves the problem of low yield due to C(sp3)–H bonds being difficult to activate, and generates C-H bonds activated by means of the ligand, thereby reducing by-products.
专利号:WO-2024182268-A1
优先权日:2023-02-27
标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics
发明人:HAN AMY
权利人:REGENERON PHARMA
摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:US-2023183223-A1
优先权日:2020-05-14
标题:Process for the synthesis of n-butyloxycarbonyl-3-(4-imidazol-1- ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide
发明人:CERNAKS DMITRIJS; DEGE ELIZA
权利人:VICORE PHARMA AB
摘要:There is provided a new process for the synthesis of compounds of formula I, which are useful as angiotensin (Ang II) type 2 receptor agonists: by reacting a compound of formula II, with an excess of a compound of formula III, wherein W, Z and X have meanings given in the description; followed by reaction of the intermediate so formed with a suitable source of the counter-ion, W.
专利号:US-2023286918-A1
优先权日:2020-07-02
标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat
发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER
权利人:AKEBIA THERAPEUTICS INC
摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.