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�ؼ���� 2-��-6-�� ϳ� Ӧ��

Abstract�� This paper reviewed the synthetic methods and applications in the pharmaceutical field of 2 amino 6 chloropurine basing on many recent document.2 Amino 6 chloropurine is an important pharmaceutical intermediate for production of the compound useful as an antiviral, anticancer, anti inflammatory and hypotensor drugs. The synthetic methods of 2 amino 6 chloropurine comprises guanine reacting by chlorine sparging, guanine reacting directly with chlorinating agent, guanine protecting by acyl group and then reacting with chlorinating agent, derivative of pyrimidine reacting with chlorinating agent thereafter ring closing etc. The last two methods were sensible for there simple industrial art, moderate operating condition and high yield.

Keywords��

Received 2001-03-15; published 2001-03-15

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ս��Ӣ,��,��.2-��-6-��ʵĺϳɷ��;[J]. ��ѧ��ҵ�빤��, 2001,18(2): 87-92

ZHAN Pei ying, FENG Ya qing,ZHANG Wei hong .Synthesis and Application of 2-Aamino-6-chloropurine[J]. Chemcial Industry and Engineering, 2001,18(2): 87-92

[1]	SAGIG ,OTVOSL ,IKEDAS ,etal.Synthesisandantiviralactivitiesof 8 alkynyl ,8 Alyenyl and8 alky1 2 deoxy adenosineahalogues[J].JMedChem ,1994 ,37:130 7 1311.
[2]	VANAERSCHOTA ,PETROSMAMOS ,PIETA .AntiviralactivityofC Alkylatedpruinenucleosidesobtainedbycrose couplingwithtetralkyltinre agents[J].JMedChem ,1993,36:2 938 2 94 2 .
[3]	MATSUDAA ,SHINOZAKIM ,YAMAGUCHIT .2 Alkynyladenosines:Anovelclassofselectivead enosisA2 receptoragonistswithpotentantihyper tensiveeffects[J].JMedChem ,1992 ,35:2 4 1 2 52 .
[4]	ESTSPKG ,JOSEFKA .Synthesisandstructure activityrelantionshipsof 6 heterocyclic substitutedpurineasinactivationmodiflersofcardiacsodiumchannels[J].JMedChem ,1995,38:2 582 2 595.
[5]	DOYLEDAVESG .PotentialpurineantagonistsXXII.Thepreparationandreactionsofcertainde rivativesof 2 amino 6 purinethiol[J].JAmChemSoc ,1960 ,82 :2 633 2 640 .
[6]	IGI,MASAMI,HAYASHI,etal.Methodforproducing 2 amino 6 halogenopuineandsynthesisintermediatetherefo [P].EP :0 543 0 95A2 ,1993 0 5 2 6.
[7]	HAMDEN ,MICHAEIRAYMOND ,JARVEST ,etal.Processfortheproparationof 2 amino 6 chlo ropurine[P].EP :0 2 0 3685A2 ,1986 0 3 2 1.
[8]	HANSON ,JOHN .Pharmaceuticals[P].WO :92 13589,1992 0 8 2 0 .
[9]	�� .6 ��ʵ��Ʊ�� [P].JP :0 52 13952 ,1993 0 8 0 5.
[10]	KILLEN ,CHRISTOPHER ,ROBERT ,etal.Preparationof 2 amino 6 chloropurine[P].WO :93 150 75,1993 0 8 0 5.
[11]	SOBOTTA ,RAINER ,RAMERT ,etal.Verfahr enzurherstellungvon 2 amino 6 chlorpurinund 2 acylamino 6 chlorpurinen[P].EP :0 684 2 4 3A1,1995 0 4 2 2 .
[12]	HANSON ,JOHN ,CHRISTOPHER .Processforthepreparationof 2 amino 6 chloropurine [P].WO :94 0 7892 ,1994 0 4 14.
[13]	STUCKY ,CERHARD .Processforproducing 2 amino 6 chioropurineandintermediatestherefor[P].WO :96 2 1664,1996 0 7 18.
[14]	��ϸ��ѧƷ�ǵ�ίԱ�� .��ҩ [M].�� :��ѧ��ҵ�� ,1996.
[15]	��ʤ ,�� .�ȴ��ʵļ��ȷ�Ӧ�о� [J].��ϸ�� ,1996,16( 5) :51 54.
[16]	KIM ,DK ,LEE ,etal.Synthesisandevaluationof 2 amine 9 ( 3 hydroxymethyl 4 alkoxycarbony loxybut 1 y1)purineaspotentialprodrugsofpenci clovir[J].JMedChem ,1998,4 1( 18) :34 35 34 4 1.
[17]	QIUYL ,JIRIZEMLICKA .Anewefficientsyn thesisofantiviralmethylenecyclopropaneanalogsofpurinenucleosides[J].Synthesis ,1998,10 :144 7 1452 .
[18]	UBASAWA ,MASARU .Preparationofphospho natenucleotidecompoundsasdrugs[P].WO :98 0 672 6,1998 0 2 19.
[19]	ANTONINHOLY ,MILENAMASOJIDKOVA .SynthesisofenantiomericN ( 2 phosphonmethox ypropyl) ,derivativesofpurineandpyrimidinebases[J].CollectCzechChemCommun ,1995,60 :1196 12 12 .
[20]	[2 0 ]SCHINAZI ,RAYMONDF .Treatmentofdrogenitalcancerwithbornnetroncapturetherapy ,andpreparationofcarboranyl containingnucleosides[P].WO :96140 73,1996 0 5 17.
[21]	LUM ,ROBERTT .Preparationofpurineinhibi torsofcyclindependentkinase 2andIKB �� ki naseforuseasantitumorantiproliferative ,andleukemiainhibitingagents[P].JP :10 0 7695,1998 0 1 13.
	[2 2 ]SANEYOSHI,MINEO .Preparationof 3�� amino 3�� deoxypurineribonucleosideasanticancerdrugs[P].JP :10 0 7695,1998 0 1 0 3.
[22]	BENSON ,BRADLEYJ .N substituted (di hydroxyboryl)alkylpurine ,indoleandpyrimidinederivativesusefulasinhibitorsofinflammatorycy tokines[P].WO :953530 0 ,1995 12 2 8.
[23]	[2 4 ]ACEVEDO ,OSCARL ,HEBERT ,etal.Combi natroriallibraryonthepreparationofpyrrolidine containingmonomersandoligomersasphospho lipaseA2 inhibitorsandanti inflammatoryagent[P].US :571460 6,1995 0 1 11.
[24]	KOBORI,TAKEO .Preparationofaminoacidderi vativeasangiotensinIVreceptoragonist[P].WO :980 562 4 ,1998 0 2 12 .
[25]	LICHEN ,NAOMISAKAI,SARAT .Towardsu pramolecularionchannelsformedbyoligonucle otitdanalogs:Hydrophobicguaninedimers [J].Tetrahedronletter,1998,39:362 7 3630 .