CAS: 7752-82-1; 5-Bromopyrimidin-2-Amine

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883231-23-0 31402-54-7 823-89-2

上下游产品

CAS号109-12-6 2-氨基嘧啶 | CAS号35034-15-2 2-Pyrimidinamin... | CAS号7664-41-7 氨 | CAS号32779-36-5 5-溴-2-氯嘧啶 | CAS号1111638-05-1 6-溴-2-甲基咪唑并[1,2-a]嘧啶 | CAS号32779-36-5 5-溴-2-氯嘧啶 | CAS号32779-37-6 2,5-二溴嘧啶 | CAS号31402-54-7 5-溴-2-甲基氨基嘧啶 | CAS号38696-21-8 5-溴-2-(二甲基氨基)嘧啶 | CAS号308348-93-8 2-氨基吡啶-5-羧酸甲酯 | CAS号402960-38-7 2-氨基嘧啶-5-硼酸频哪醇酯 | CAS号38353-06-9 5-溴-2-羟基嘧啶 | CAS号936250-22-5 2-氨基嘧啶-5-硼酸 | CAS号478258-81-0 5-溴-2-(2,5-二甲基-...

2-氨基吡啶置于n-溴代丁二酰亚胺(Nbs)体系中,用 乙腈 作为反应溶剂,以97%的收率获得产物2-氨基-5-溴嘧啶
参考文献:Discovery Of (R)-5-((5-(1-Methyl-1H-Pyrazol-4-yl)-4-(Methylamino)Pyrimidin-2-yl)Amino)-3-(Piperidin-3-Yloxy)Picolinonitrile,A Novel Chk1 Inhibitor For Hematologic Malignancies
标题:Discovery Of (R)-5-((5-(1-Methyl-1H-Pyrazol-4-yl)-4-(Methylamino)Pyrimidin-2-yl)Amino)-3-(Piperidin-3-Yloxy)Picolinonitrile,A Novel Chk1 Inhibitor For Hematologic Malignancies
摘要:Through Virtual Screening,We Identified The Lead Compound Mcl1020,Which Exhibited Modest Chk1 Inhibitory Activity. Then A Series Of 5-(Pyrimidin-2-Ylamino)Picolinonitrile Derivatives As Chk1 Inhibitors Were Discovered By Further Rational Optimization. One Promising Molecule. (R)-17,Whose Potency Was One Of The Best,Had An Ic50 Of 0.4 Nm With Remarkable Selectivity (>4300-Fold Chk1 Vs. Chk2). Compound (R)-17 Effectively Inhibited The Growth Of Malignant Hematopathy Cell Lines Especially Z-138 (Ic50: 0.013 Mu M) And Displayed Low Affinity For Herg (Ic50> 40 Mu M). Moreover,(R)-17 Significantly Suppressed The Tumor Growth In Z-138 Cell Inoculated Xenograft Model (20 Mg/kg I.V.,Tgi = 90.29%) As A Single Agent With Body Weight Unaffected. Taken Together,Our Data Demonstrated Compound (R)-17 Could Be A Promising Drug Candidate For The Treatment Of Hematologic Malignancies. (C) 2019 Published By Elsevier Masson Sas.
DOI:10.1016/j.Ejmech.2019.03.062

专利信息

专利号:WO-9740052-A1
优先权日:1996-04-22
标题 :Propagylglycine derivatives, preparation and utilisation thereof as synthesis intermediates
发明人：CARDINAUD ISABELLE; CHEKROUN ISAAC; ROSSEY GUY; CREMER GERARD; GOBERVILLE PASCALE; HOORNAERT CHRISTIAN
权利人:SYNTHELABO; CARDINAUD ISABELLE; CHEKROUN ISAAC; ROSSEY GUY; CREMER GERARD; GOBERVILLE PASCALE; HOORNAERT CHRISTIAN
摘要:Compounds of formula (I) wherein R2 is -CH2C=CH or -CH2C=C-Het where Het is a 2-aminopyridyl, 2-aminopyrimidyl, 6-aminopyridazinyl, imidazol-4-yl group, R3 and R4 each represent hydrogen, (C1-C4)alkyl, (C1-C4)alkoxycarbonyl, ArCH2CO2- or ArSO2- where Ar is an aryl group, or a group (a) where R7 is hydrogen or -COR, R being straight or branched (C1-C7) alkyl, -(CH2)nOCH3 or -CH2O(C2H4O)nCH3 (n is 1, 2 or 3) and A is chosen among the phenyl, pyrimidyl, pyridinyl, thienyl, thiazolyl and furyl groups, R6 represents either a straight or branched (C1-C4) alkoxy group, or a benzyloxy group or a group (b) where R12 is a hydrogen atom or a carboxylic or (C1-C4)alkoxycarbonyl group and R13 is a straight or branched (C1-C4)alkyl group. They constitute synthesis intermediates.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-2010286211-A1
优先权日:2004-10-08
标题:Oxazolidinone derivatives as antimicrobials
发明人：DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK
权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK
摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

专利号:US-6852711-B2
优先权日:1998-09-11
标题:HIV protease inhibitors
发明人：BOYER JR FREDERICK EARL; DOMAGALA JOHN MICHAEL; ELLSWORTH EDMUND LEE; GAJDA CHRISTOPHER ANDREW; HAGEN SUSAN ELIZABETH; LOVDAHL MICHAEL JAMES; LUNNEY ELIZABETH ANN; MARKOSKI LARRY JAMES; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN
权利人:AGOURON PHARMA
摘要:The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-7002020-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.