丙酰氯置于磺酰氯,碘体系中,化学反应生成 2-氯丙酰氯 参考文献:Kharasch; Brown,Journal Of The American Chemical Society,1940,Vol. 62,P. 928 标题:Kharasch; Brown,Journal Of The American Chemical Society,1940,Vol. 62,P. 928
专利号:WO-2020246902-A1 优先权日:2019-06-07 标 题 :An initiator of atrp radical polymerisation, a method of its synthesis, and a method of synthesis of low-dispersion polymer and copolymer using this initiator 发明人:MEGIEL ELÅ»BIETA; ROMAŃSKI JAN; FEDORCZUK MAGDALENA 权利人:UNIV WARSZAWSKI 摘要:An initiator of ATRP radical polymerisation having a functional group with a substituent active in polymerisation process, is characterised in that it is a bifunctional initiator containing at least two functional groups separated by a hydrocarbon moiety Y, where the first functional group has an active substituent X and the second functional group has a protecting group Z, which can be chemically modified with the same or a different substituent than the active substituent X present in the first functional group. A method of synthesis of 2-chloro-N-(2-hydroxyethyl)propionamide initiator, NCPAE, is characterised in that ethanolamine is subjected to an acylation reaction with 2-chloropropionyl chloride in presence of triethylamine (TEA), wherein the reaction is carried out under inert atmosphere at room temperature.
专利号:EP-4423083-A2 优先权日:2021-11-29 标 题:Synthesis of pyrazolone derivative compounds and their effects on cox enzymes 发明人:ÖNAY UÇAR EVREN; DEM RAYAK EREF; BERK BARKIN; YURTTA LEYLA; B LTEK N KALEL SEVDE NUR; AH N ZAFER 权利人:UNIV ISTANBUL MEDIPOL; ISTANBUL UNIV REKTORLUGU; ANADOLU UNIV 摘要:The invention is related to the synthesis of 8 pyrazolone derivative compounds and their activities on COX enzymes.
专利号:WO-9946267-A1 优先权日:1998-03-12 标题 :Modulators of protein tyrosine phosphatases (ptpases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS; ONTOGEN CORP 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:WO-2014202765-A1 优先权日:2013-06-21 标题 :Preparation of chiral 1-methyl-2,3,4,5-1h-benzodiazepines via asymmetric reduction of alpha-substituted styrenes 发明人:STAVBER GAJ; GAZIC SMILOVIC IVANA; CLUZEAU JEROME; RICHTER FRANK 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides an asymmetric and economic synthesis of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H-benzo[d]azepine via novel intermediates applying an asymmetric enzymatic, biomimetic or catalytic reduction. The present invention also provides a novel green asymmetric catalytic reduction adapted for an aqueous medium to be applied in the synthesis of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H-benzo[d]azepine or novel intermediates.
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
参考标题:Synthesis Of Poly-Functionalized Pyrazoles Under Vilsmeier-Haack Reaction Conditions 作者:Aleksandr V. Popov,Valentina A. Kobelevskaya,Ludmila I. Larina,Igor B. Rozentsveig 摘要:Synthesis Of 1,3-Disubstituted 5-Chloro-1H-Pyrazole-4-Carbaldehydes Was Achieved By Formylation Of The Corresponding 5-Chloro-1H-Pyrazoles Under Vilsmeier-Haack Conditions.
合成参考文献
参考文献:10.1007/s00044-016-1731-7 摘要:Martirosyan AH, Gasparyan SP, Alexanyan MV, Harutyunyan GK, Panosyan HA, Schinazi RF. Anti-human immunodeficiency activity of novel 2-arylpyrrolidine analogs. Medicinal Chemistry Research. 2016 Oct 17;26(1):101–8. doi: 10.1007/s00044-016-1731-7.