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1、S- ( - ) -:)李null 谢null 杜有国null 宗在伟null 陈祥峰(2Z;,2210009)Knull1null 5-J- 2- (4-J- 3, 5-=J- 2-J)J; - 1H -&i,:Vsd&QS- ( - )-:,_)QS- (- ) -:)b1oMnull S- ( - ) -:)null0,4nullnulll: 2008- 12- 15Te:(1984 ),3,=,VY07?Tnull Research of Synthesis of S- (- ) - Omeprazole SodiumLiXienull DuYouguonull Zong Zaiwei
2、null ChenXiangfeng(NanjingHaiGuang Institute ofApplied Chemistry, JiangsuNanjing 210009)Abstractnull S- (- ) - omeprozolewas prepared from 5- mehtoxy- 2- (4- methoxy- 3, 5- dimethyl- 2-pyridinyl) methylthio benzimidazole and cumene hydroperoxide by asymmetric oxidation. The productwas reactedwith so
3、dium hydroxide to give S- (- )- omeprozole sodium.Keywordsnull S- (- )- omeprazolenull proton pump inhibitornull synthesisnull null S- (- ) -:)(Esomeprazole Sodium),S- (- )- 5-J- 2- (4-J- 3, 5-=J- 2-J)J - 1H-&i,:),n50,4:B8S- ( - ) -:)b01aE=ahJ5#b5Xh8R-:, S-:rzaT1bS- (- ) -:)V,eZE!8cS-:1obD2 4ZE1/3:n
4、ullmsk4ZEh8:s,.dsZE4r:1as,7OZEn1/2:; null3ZE,P3:;:+,:B8,ZE1LLZE,VNP; nullZE,Pmb4!m1null S- ( - ) -nullU)LScheme. 1null the synthesis route ofS- ( - ) - omeprozolenull35null2322009M2null null null null null null null null null nullHChem ical Industry Tmi esnull null null null null null null null null
5、 nullVo.l 23, No. 2Feb. 2. 2009:B8,ZEM-ZLb7-D 5ZES- ( - )-:8:sd?aD- (- )-F=Ya=sdY8b/jV_:;S-:b=sdYNL,av31pbYVQL,Pa1eQHq/!S-:,7S- (- ) -:)bLnm1b1Ls1. 1nullN!ZF- 6,LsN; YRT- 3N;LC- 10TvprAMN; Varian INOVA 500HN(TMS=S, COCl3DMSO- d64)b1. 2nullLZE1. 2. 1null S- ( - ) -奥美拉唑的合成gGQF5-J- 2- (4-J- 3, 5-=J- 2-
6、J)J; -1H-&i,:57gaYY20mL,B1. 1mLaD- ( - )-F=Y30. 5mLsd?(null),50nullQ1h,30null ,FY15. 5mLVsd&24. 5mLb/iQ2hbF12%AY|,iM,iYpH7,YYY|,iM,;)2,Vr,hi5TbHPLCsB98. 5%,;B95. 7% e. e.(HPLC_:mAGP,Y-)AM; C18AoAA,Y-=_)AM), 1HNMR(CDCl3) null: 2. 18( s, 3H), 2. 21(s, 3H), 3. 67( s, 3H), 3. 83( s, 3H), 4. 75(m, 2H),6.
7、 94(dd, 1H), 7. 0(b, 1H), 7. 5(b, 1H), 8. 2(s, 1H)b1. 2. 2null S- ( - ) -奥美拉唑钠的合成|Q5250mL,Hq/F_)A,iQ10m in,FJ&,v%8,Vr,Y!,2x%832. 3 gb9lq: 50. 8%,mp: 248 250null (s) (D5:lq46%; mp: 247 249null ), HPLCsB99. 4%,;B99. 5% e. e. ( HPLC_:mAGP,Y-)AM; C18AoAA,Y-=_)AM), nullD20 + 43. 8null( c0. 5%) (D6: nullD
8、 20 + 44. 1null), 1HNMR(CDCl3) null: 2. 20(s, 3H), 2. 21(s, 3H), 3. 68( s, 3H),3. 71( s, 3H), 4. 37(d, 1H), 4. 75(d, 1H), 6. 53(dd,1H), 6. 96(d, 1H), 7. 3(d, 1H), 8. 21(s, 1H)b2T)null null5-J- 2- (4-J- 3, 5-=J- 2-J)J; - 1H -&i,:,S- (- )-:)Q,YVYBa9=sdY;?PQzVvvbYVQ5-J- 2- (4-J- 3, 5-=J- 2-J)J -1H-&i,:
9、B/BQ,;eT,hBVbVhP,hl4bI,S- (- )-:H,iYPlqvY,ApHl6H,4(:+)3;pHv8H,5lqv/bID1nulla,+,k*. S-:ME J., 2000, 10: 193 1942nullS,ulC,+.84!(S) -:ZE P.S?,#h|:200610023955. 4, 2006- 0l- 283null A Grau,l R Castaber, JCastaber. Esomeprazolemagnesium J. Drug ofthe Futrue, 1999, 24(11): 1178 11834null JingenDeng. Resolution of omeprazole by inclusion co
