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参考文献:使用基于环戊达[g]喹唑啉的胸苷酸合酶抑制剂靶向α-叶酸受体.
标题:使用基于环戊达[g]喹唑啉的胸苷酸合酶抑制剂靶向α-叶酸受体.
摘要:据报道,α-Fr在许多癌中过表达,特别是在卵巢癌和子宫癌中.在过去的十年中,已经利用α-Fr在某些肿瘤中与正常组织中的高表达来将叶酸介导的大分子,抗癌药,显像剂和核酸靶向癌细胞.据报道,Cb300638是一种基于环戊基[g]喹唑啉的胸苷酸合酶(ts)抑制剂,对受体具有高亲和力,并且对过表达α-Fr的肿瘤细胞系具有高度选择性.在这项研究中,针对ts抑制作用,研究了分子的结构特征,尤其是在2位修饰的分子,与新转染的a431细胞相比,A431-Fbp细胞(用人α-Fr转染)对α-Fr的亲和力和降低的叶酸载体(rfc)和活性.利用多步序列合成了化合物1A,B,2A,B和3A,B.发现2-取代基不影响对α-Fr的亲和力;反之,α-Fr不受影响.但是,它极大地影响了对a431-Fbp细胞的选择性,并表明除了ts抑制作用和α-Fr亲和力以外,还有其他因素对于这些化合物的活性也很重要.与a431细胞相比,
Doi:10.1016/j.Bmc.2006.03.001
专利信息
专利号:US-5648537-A
优先权日:1995-01-24
标题 :Process for the synthesis of substituted carbodiimides
发明人:HUSSENET PATRICIA; LE GOFF PHILIPPE; SENNYEY GERARD
权利人:POUDRES & EXPLOSIFS STE NALE
摘要:The invention relates to a new process for the synthesis of a disubstituted carbodiimide, including a first stage of phosgenation of an N,N'-disubstituted urea in an organic solvent medium. n After this first stage ammonia is added to the reaction mixture without preliminary isolation of any intermediate compound. n The process is simple, relatively inexpensive and the yield is high. n Disubstituted carbodiimides are organic synthesis intermediates used especially in pharmaceutical chemistry as coupling agents in peptide synthesis.
专利号:US-5919971-A
优先权日:1996-11-22
标题:Process for the synthesis of 3-mercaptopropionic acid esters
发明人:ARRETZ EMMANUEL
权利人:ELF AQUITAINE EXPLORATION PROD
摘要:This process for the synthesis of 3-mercaptopropionic acid esters by addition reaction of H2S to the corresponding acrylic acid ester is carried out in the presence of a solid-support functionalized with basic guanidine functional groups, on condition that these groups are free of hydrogen that is directly attached to a nitrogen atom.
专利号:US-5877349-A
优先权日:1996-09-20
标 题:Process for the synthesis of 3-mercaptopropionic acid
发明人:ARRETZ EMMANUEL
权利人:ELF ACQUITAINE EXPLORATION PRO
摘要:This process for the synthesis of 3-mercaptopropionic acid by an addition reaction of H 2 S with acrylic acid is carried out in the presence of a solid support having basic guanidine functional groups, provided that the latter do not contain hydrogen bonded directly to a nitrogen atom.
专利号:US-7256197-B2
优先权日:2001-10-12
标 题 :Methods for synthesis of diarylmethanes
发明人:ROSOWSKY ANDRE; CHEN HAN
权利人:DANA FARBER CANCER INST INC
摘要:The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; methods of preparation of dihydrofolate reductase inhibitors that include metal mediated cross coupling of an aromatic halide or heteroaromatic halide with an organozinc reagent; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such dihydrofolate reductase inhibitors.
专利号:US-5712407-A
优先权日:1997-01-14
标题 :Method for the preparation of alpha-chlorinated chloroformates
发明人:KREUTZBERGER CHARLES B; ESWARAKRISHNAN SEETHA; DAMLE SURESH B
权利人:PPG INDUSTRIES INC
摘要:Novel catalysts for the synthesis of a alpha-chlorinated chloroformate from an aldehyde and phosgene are described. The catalysts include alkyl substituted guanidines, hexasubstituted guanidinium chlorides, substituted biguanidinium chloride, phenyldialkyliminiumtetraalkylguanidinium chloride, dialkylimidazolinium tetraalkylguanidinium chloride, phenyltetraalkylamidinium chloride and N,N-dialkyl-N'-alkylpyrrolidinium chloride.
专利号:WO-2021078995-A1
优先权日:2019-10-25
标 题 :Selective polypeptide synthesis stalling assay and compound
发明人:STROUS GERARDUS JACOBUS ANTONIUS MARIA; MOL JAN ADRIANUS; VAN DER VELDEN LIEKE MARIE; KLUMPERMAN JUDITH; MAAS PETRUS EMMANUEL MARIE; PIET DENNIS PATRICK; DE KLERK-SPRENKELS NANDA ELISABETH; TIJHUIS JOHANN HEINRICH; VIÉTOR HENDRIK ENGELBERTUS; MAURICE MADELON MARIA; VAN DER KRIFT FELIX
权利人:UMC UTRECHT HOLDING BV; UNIV UTRECHT HOLDING BV; BIMINI BIOTECH B V
摘要:The invention relates to compounds, in particular pyrimidine-2,4-diamines, analogues and salts thereof and pharmaceutical compositions comprising pyrimidine-2,4-diamines analogues and salts thereof for use in the treatment and prevention of a disease, in particular a growth hormone receptor-dependent condition. The invention also relates to methods of using these compounds and compositions to treat physiological disorders related to the amount or activity of growth hormone. In a particular embodiment, the invention relates to a compound according to formula 1 for use in the treatment or prevention of a disease in a subject.