专利号:US-12441721-B2 优先权日:2020-07-21 标 题 :Synthesis of heterocyclic compounds from carboxamide and carboxamide derivatives with haloalkanols 发明人:KARPOORMATH RAJSHEKHAR; SAYYAD NISAR 权利人:UNIV OF KWAZULU NATAL 摘要:The invention provides for methods for the synthesis of various compounds through reaction of carboxamide, or carboxamide derivatives, with various substituted or unsubstituted haloalkanols in a one-step, single vessel, reaction mechanism. Preferably, but not exclusively, the reaction proceeds in the absence of any solvents, catalyst, base, or any further reagents.
专利号:WO-2011101864-A1 优先权日:2010-02-17 标题 :Novel process for the synthesis of phenoxyethyl derivatives 发明人:JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 权利人:PANACEA BIOTEC LTD; JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 摘要:The present invention provides an improved process for the synthesis of 2-[2- (2,2,2-trifluoroethoxy)phenoxy]ethanol intermediate, its derivatives and/or its pharmaceutically acceptable salts, useful in the synthesis of α-1 adrenoceptor blockers such as silodosin.
专利号:US-5436143-A 优先权日:1992-12-23 标题:Method for enzymatic synthesis of oligonucleotides 发明人:HYMAN EDWARD D 摘要:Enzymatic synthesis of oligonucleotides may be performed in a single vessel without intermediate purification, by the steps of: n (a) combining a nucleotide primer sequence and a blocked nucleotide in the presence of a chain extending enzyme whereby a reaction mixture is formed containing the blocked nucleotide coupled to the nucleotide primer sequence at its 3' end; n (b) inactivating the chain extending enzyme; n (c) removing the blocking group from the primer-blocked nucleotide to form a primer-nucleotide product; and converting any unreacted blocked nucleotide to an unreactive form which is substantially less active as a substrate for the chain extending enzyme than the blocked nucleotide.
专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-9975832-B2 优先权日:2014-12-29 标题:Process for the preparation of ospemifene and fispemifene 发明人:CRISTIANO TANIA; ALPEGIANI MARCO 权利人:OLON SPA 摘要:Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH 2 CH 2 —Y of formula 7, wherein X is a leaving group and Y is the —(OCH 2 CH 2 ) n OH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
[参考文献]: David M Hodgson, Et Al. Stereocontrolled Syntheses Of Kainoid Amino Acids From 7-Azabicyclo[2.2.1]Heptadienes Using Tandem Radical Addition-Homoallylic Radical Rearrangement. J Org Chem. 2005 Oct 28;70(22):8866-76.
合成参考文献
摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2022) 2, 32. 摘要:Grimmer, J.; Krieg, S.-C.; Manolikakes, G., Science of Synthesis Knowledge Updates, (2021) 1, 231. 摘要:Hata, S.; Sibi, M. P., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 896. 摘要:Yorimitsu, H.; Oshima, K., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 666.