4,6-二氯嘧啶置于乙醇,氨体系中,化学反应生成4,6-二氨基嘧啶 参考文献:Kenner Et Al.,Journal Of The Chemical Society,1943,P. 574 标题:Kenner Et Al.,Journal Of The Chemical Society,1943,P. 574
专利信息
专利号:US-7105666-B2 优先权日:2002-06-27 标 题:Synthesis of purine derivatives 发明人:HAMMARSTROEM LARS G J; KRAUSS NANCY ELISABTH; LABADIE SHARADA SHENVI; SMITH DAVID BERNARD; TALAMAS FRANCISCO XAVIER 权利人:ROCHE PALO ALTO LLC 摘要:The present invention provides a method for producing 2-, 6-, 8- and 9-substituted purine compounds from 4,6-dihalo-5-nitro-2-alkyl-pyrimidine compounds in solution or by solid phase techniques. The present process provides for the sequential introduction of amine substituents at the 4- and 6-positions, displacement of an alkylsulfony group at the 2-position of the pyrimidine, reduction of the nitro group and formation of the imidazole portion of the purine compound. Furthermore, the methods of the present invention are ideally suited to the preparation of a library of purine compounds.
专利号:US-3940393-A 优先权日:1974-06-21 标题 :Synthesis of 2,6-diaminopyrimidines 发明人:GREENSPAN GEORGE; REES RICHARD W; RUSSELL PETER B 权利人:AMERICAN HOME PROD 摘要:New, substituted, 2,6-diaminopyrimidines are disclosed. These compounds are useful as anti-malarial agents. The oxygenation of pyrimethamine by fungi is also disclosed.
专利号:US-2006025327-A1 优先权日:2004-07-30 标 题 :Hybrid molecules QA, wherein Q is an aminoquinoline and a is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent 发明人:SANCHEZ MURIEL; MEUNIER BERNARD 权利人:PALUMED S A & CT NAT DE LA REC 摘要:Aminoquinoline-antibiotic hybrid compounds in the form of hybrid molecules QA, wherein Q is an aminoquinoline and A is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent. This compound is defined by the general formula (I): n nQ-(Y 1 ) p —(U) p′ —(Y 2 ) p″ -A  (I) nin which n Q represents an aminoquinoline, (Y 1 ) p —(U) p′ —(Y 2 ) p″ — is an optional spacer arm and A is an antibiotic, one of its derivatives or precursors, or a resistance enzyme inhibitor. The invention unexpectedly enables the activity of the antibiotic to be improved.
专利号:US-10981958-B2 优先权日:2016-12-06 标 题 :Peptide modulator of purinergic receptors 发明人:VASSILEVSKI ALEXANDER ALEXANDROVICH; OPARIN PETER BORISOVICH; Korolkova Yuliya Vladimirovna; Mosharova Irina Vladimirovna; SAVCHENKO GANNA ANATOLIEVNA; BOYCHUK YAROSLAV ANATOLIEVICH; KRISHTAL OLEG ALEXANDROVICH 权利人:“FUTURE ANALGESICSâ€? LTD 摘要:The invention refers to medicine and pharmacology, namely, to biologically active peptides, which modulate purinergic signaling. For that, the peptide with the following amino acid sequence is proposed: n n n n n n Gly 1 -Tyr 2 -Cys 3 -Ala 4 -Thr 5 -Lys 6 -Gly 7 -Ile 8 -Lys 9 -Cys 10 - n n n n Asn 11 -Asp 12 -Ile 13 -His 14 -Cys 15 -Cys 16 -Ser 17 -Gly 18 -Leu 19 - n n n n Lys 20 -Cys 21 -Asp 22 -Ser 23 -Lys 24 -Arg 25 -Lys 26 -Val 27 -Cys 28 - n n n n Val 29 -Lys 30 -Gly 31 , n n n n n n n n n n n n n n n n n or a sequence with at least 90% homology hereto. n Peptides in the invention can be used for prevention and treatment of diseases mediated by purinergic receptors. The peptides can be used for development of new drugs on their basis, for example, analgesics, as well for investigation of mechanisms of pain occurrence, for identification and testing of new modulators of P2X3 receptors. The peptides in the invention can be produced using chemical synthesis or biotechnologically using the nucleotide sequence of the corresponding gene.
专利号:EP-3686190-A1 优先权日:2013-07-11 标 题 :Synthesis of therapeutically active compounds
专利号:CA-2488562-A1 优先权日:2002-06-27 标 题:Synthesis of purine derivatives