专利号:US-11459303-B2 优先权日:2019-06-21 标题 :Process for the synthesis of lofexidine 发明人:DONNOLA MONICA; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.
专利号:US-6162882-A 优先权日:1996-07-10 标 题:Preparation of novel homo- and copolymers using atom transfer radical polymerization 发明人:MATYJASZEWSKI KRZYSZTOF; COCA SIMION; GAYNOR SCOTT G; NAKAGAWA YOSHIKI; JO SEONG MU 权利人:UNIV CARNEGIE MELLON 摘要:The present invention is directed to a process of atom (or group) transfer radical polymerization for the synthesis of novel homopolymer or a block or graft copolymer, optionally containing at least one polar group, with well defined molecular architecture and narrow polydipersity index, in the presence of an initiating system comprising (i) an initiator having a radically transferrable atom or group, (ii) a transition metal compound, and (iii) a ligand, the present invention is also directed to the synthesis of a macromolecule having at least two halogen groups which can be used as a macroinitiator component (i) to subsequently form a block or graft copolymer by an atom or group transfer radical polymerization process; the present invention is also directed to a process of atom or group transfer radical polymerization for the synthesis of a branched or hyperbranched polymer; in addition, the present invention is directed to a process of atom or group transfer radical polymerization for the synthesis of a macroinitiator which can subsequently be used to produce a block or graft copolymer.
专利号:US-2013165350-A1 优先权日:2011-12-22 标 题:Surface linkers for array synthesis 发明人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR 权利人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR; AFFYMETRIX INC 摘要:The present invention provide several methods of derivatizing a surface of a support with one or more linkers thus providing a suitable platform for synthesis of a polymer array, particular a nucleic acid array. Some methods derivatize a surface with a self-assembled monolayer (SAM) of a linker. The SAM confers advantages of hydrolytic stability, broad compatibility with synthesis and detection chemistries, and reduced emergence of latent functional groups during polymer array synthesis. Substrates can also be derivatized with multi-layers of SAMs providing greater hydrolytic stability. Substrates can also be derivatized by synthesizing a linker in situ on the substrate by atom transfer radical polymerization of functional and functional monomers. Appropriate selection of monomers reduces emergence of latent functional groups in subsequent array synthesis.
专利号:US-12053529-B2 优先权日:2018-08-01 标题:Amino-reactive positively charged ATRP initiators that maintain their positive charge during synthesis of biomacro-initiators 发明人:RUSSELL ALAN J; MURATA HIRONOBU 权利人:UNIV CARNEGIE MELLON 摘要:Provided herein are materials and methods that include utilizing atom transfer radical polymerization (ATRP) initiator molecules that maintain a positive charge during biomacro-initiator synthesis.
专利号:US-5856501-A 优先权日:1997-03-11 标题 :Synthesis of thiazole derivatives 发明人:MALCOLM ARCELIO J; WU TSE-CHONG 权利人:ALBEMARLE CORP 摘要:N- 4-(cyanoethylthiomethyl)-2-thiazolyl!guanidine--a key intermediate for preparing the pharmaceutical, famotidine--is produced by mixing in a liquid medium formed from a chemically indifferent organic solvent and water, and under an inert atmosphere, (i) a 2-guanidino-4-halomethylthiazole or a hydrohalide complex thereof, (ii) an S-(2-cyanoethyl)isothiourea or a hydrohalide complex thereof, and (iii) a strong alkali metal base. In lieu of (ii), an alkali metal salt of 2-cyanoethyl-1-thiol can be used, and in such case use of (iii) is optional, but preferable.
专利号:US-5281725-A 优先权日:1991-10-07 标 题:Derivatives of 2,2-dihalogenobenzo[1,3]dioxoles substituted in the 4-position, processes for their preparation and their use 发明人:ANDRES PETER; MARHOLD ALBRECHT 权利人:BAYER AG 摘要:New 2,2-dihalogeno-benzo[1,3]dioxoles substituted in the 4-position, of the general formula (I) ##STR1## in which R represents fluorine, chlorine, bromine or nitro and n Hal represents chlorine or fluorine, and their use as starting substances for the synthesis of highly active compounds, for example in the field of plant protection and pharmaceuticals. n The compounds of the formula (I) can be prepared by analogous processes, for example by chlorination from corresponding benzo[1,3]dioxoles substituted in the 4-position, and these substances according to the invention can be further reacted with hydrogen fluoride to give substances to which the invention likewise relates.
参考标题:Reinvestigation Of The Reaction Of Trichloroacetyl Chloride And Acrylonitrile In The Preparation Of 3,5,6-Trichloropyridin-2-Ol 作者:H. Fakhraian,A. Moghimi,A. Bazaz,H. Hadj-Ghanbary,M. Sadeghi |发布日期:2003.5.1 摘要:The Synthesis Of 3,5,6-Trichloropyridin-2-Ol Via The Cucl-Catalyzed Reaction Of Trichloroacetyl Chloride And Acrylonitrile Under Both Pressure And Atmospheric Conditions And The Hydrolysis Of The Reaction Mixture Were Reinvestigated. The Products And Byproducts Formed In Each Case, Before The Hydrolysis Step, Were Characterized, And The Factors Causing Their Formation Are Discussed. It Was Found That
合成参考文献
摘要:Schiltz, P.; Gosmini, C., Science of Synthesis: Special Topics, (2021) 1, 84. 摘要:Wang, C.; Yang, F., Science of Synthesis: Special Topics, (2022) 1, 452. 参考文献:10.1021/jp061241h 摘要:Kowalczyk TD, Abrams ML, Crawford TD. Ab initio optical rotatory dispersion and electronic circular dichroism spectra of (S)-2-chloropropionitrile. J Phys Chem A. 2006 Jun 22;110(24):7649–54. doi: 10.1021/jp061241h.