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1. 发明专利

JP2008239621A Method for producing oxazolidinone 审中-公开
标题翻译：生产氧杂环丁酮的方法
公开(公告)号：JP2008239621A
公开(公告)日：2008-10-09
申请号：JP2008053675
申请日：2008-03-04
申请人： Pharmacia & Upjohn Co Llc , ファルマシア・アンド・アップジョン・カンパニー・エルエルシー
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
CPC分类号： C07D487/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10
摘要： PROBLEM TO BE SOLVED: To provide a method for producing 5-hydroxymethyl-substituted oxazolidinone alcohol and a method for forming 5-acylamide methyl-substituted oxazolidinone with antimicrobial activity by converting the 5-hydroxymethyl-substituted oxazolidinone alcohol to 5-aminomethyl-substituted oxazolidinone amine and acylating the amine derivative. SOLUTION: 5-Hydroxymethyl-substituted oxazolidinone alcohol is produced from carbamate or a trifluoroacetamide by using a dihydroxy compound or glycidol as a starting material and the hydroxymethyl-substituted oxazolidinone alcohol is converted to 5-aminomethyl-substituted oxazolidinone amines, which is then acylated to form the 5-acylamidomethyl-substituted oxazolidinone. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供5-羟甲基取代的恶唑烷酮醇的制备方法和通过将5-羟甲基取代的恶唑烷酮醇转化为5-氨基甲基的方法，形成具有抗微生物活性的5-酰基酰胺甲基取代的恶唑烷酮 - 取代的恶唑烷酮胺并酰化胺衍生物。解决方案：通过使用二羟基化合物或缩水甘油作为起始原料，由氨基甲酸酯或三氟乙酰胺制备5-羟基甲基取代的恶唑烷酮醇，将羟甲基取代的恶唑烷酮醇转化为5-氨基甲基取代的恶唑烷酮胺，其为然后酰化形成5-酰氨基甲基取代的恶唑烷酮。版权所有（C）2009，JPO＆INPIT

2. 发明专利

PT1114819E PROCESSO PARA PREPARAÇÃO DE OXAZOLIDINONAS 未知
公开(公告)号：PT1114819E
公开(公告)日：2008-02-28
申请号：PT01302264
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J , BARBACHYN MICHAEL R , PERRAULT WILLIAM R
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00

3. 发明专利

SI1114819T1 Postopek za pripravo oksazolidinonov 未知
公开(公告)号：SI1114819T1
公开(公告)日：2008-06-30
申请号：SI9730779
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/00 , C07D413/00 , C07D487/00

4. 发明专利

ES2298198T3 PROCEDIMIENTO PARA PREPARAR OXAZOLIDINONAS. 未知
公开(公告)号：ES2298198T3
公开(公告)日：2008-05-16
申请号：ES01302264
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： Un procedimiento para la preparación de una oxazolidinonamina 5-aminometilsustituida de fórmula (VII) (Ver fórmula) en la que R1 es (Ver fórmula) en la que X1 es H o F, en la que X2 es H o F en la que Q1 es: (Ver fórmulas) Q1 y X2 juntos son: (Ver fórmula) en las que Z1 es: (a) -CH2-, (b) -CH(R4)-CH2-, (c) -C(O)- o (d) -CH2CH2CH2-; en las que Z2 es: (a) -O2S-, (b) -O-, (c) -N(R7)-, (d) -OS- o (e) -S-; en las que Z3 es: (a) -O2S-, (b) -O-, (c) -OS- o (d) -S-; en las que A1 es: (a) H o (b) CH3; en las que A2 es: (a) H, (b) HO-, (c) CH3-, (d) CH3O-, (e) R2O-CH2-C(O)-NH-, (f) R3O-C(O)-NH-, (g) alquilo(C1-2)-O-C(O)-, (h) HO-CH2-, (i) CH3O-NH-, (j) alquilo(C1-3)-O2C-, (k) CH3-C(O)-, (l) CH3-C(O)-CH2-, (m) (Ver fórmula) (n) (Ver fórmula) A1 y A2 juntos son: (a) -O-CHR12-CH2-O-, (b) O=, (c) R14-N=, en las que R2 es: (a) H, (b) CH3-, (c) fenil-CH2- o (d) CH3C(O)-; en las que R3 es: (a) alquilo(C1-3) o (b) fenilo; en las que R4 es: (a) H o (b) HO-; en las que R5 es: (a) H, (b) alquilo(C1-3), (c) CH2=CH-CH2- o (d) CH3-O-(CH2)2-; en las que R6 es: (a) CH3-C(O)-, (b) H-C(O)-, (c) Cl2CH-C(O)-, (d) HOCH2-C(O)-, (e) CH3SO2-, (f) (Ver fórmula) (g) F2CHC(O)-, (h) (Ver fórmula) (i) H3C-C(O)-O-CH2-C(O)-, (j) H-C(O)-O-CH2-C(O)-, (k) (Ver fórmula) (l) HCequivCH-CH2O-CH2-C(O)- o (m) fenil-CH2-O-CH2-C(O)-; en las que R7 es: (a) R2O-C(R10)(R11)-C(O)-, (b) R3O-C(O)-, (c) R8-C(O)-, (d) (Ver fórmula) (e) (Ver fórmula) (f) H3C-C(O)-(CH2)2-C(O)-, (g) R9-SO2-, (h) (Ver fórmula) (i) HO-CH2-C(O)-, (j) R16-(CH2)2-, (k) R13-C(O)-O-CH2-C(O)-, (l) (CH3)2N-CH2-C(O)-NH-, (m) NC-CH2- o (n) F2CH-CH2-; en las que R8 es:...

5. 发明专利

DE69738457D1 未知
公开(公告)号：DE69738457D1
公开(公告)日：2008-02-21
申请号：DE69738457
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： A 5-aminomethyl-substituted oxalidine amide is prepared by reacting a 5-hydroxymethyl-substituted oxazolidinone alcohol with a sulfonylating agent, and reacting the resultant oxazolidinone sulfonate ammonia. The sulfonates are new conpounds.

6. 发明专利

RU2176643C2 METHOD OF SYNTHESIS OF 5-HYDROXYMETHYL-SUBSTITUTED OXAZOLIDINONES, METHOD OF SYNTHESIS OF 5-AMINOMETHYL-SUBSTITUTED OXAZOLIDINONE AMINES, OXAZOLIDINONE SULFONATE 未知
公开(公告)号：RU2176643C2
公开(公告)日：2001-12-10
申请号：RU98120398
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/20 , C07D263/24 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： organic chemistry, chemical technology. SUBSTANCE: invention relates to method of synthesis of 5-hydroxymethyl-substituted oxazolidinones of the formula (III) from carbamates of the formula (IIa) R1-NH-COOM2 (IIa) or trifluoroacetamide of the formula (IIb) R1-NH-CO-CF3 (IIb) using dihydroxy-compound of the formula (I) M1-CH2-CH(OH)-CH2-OH (I) or glycidol as the parent substance. Invention relates to also a method of synthesis of 5-aminomethyl-substituted oxazolidinone amines of the formula (VII) by interaction of 5-hydroxy-methyl-substituted oxazolidinones of the formula (III) with sulfonating agent and the following interaction of synthesized oxazolidinone sulfonate of the formulas (VIa),(VIb) , (VIc) , (VId) with ammonia under pressure less than 207 kPa (2.1 ati). Invention relates to also new derivatives of oxazolidinone sulfonate of the formula (VIa - VIb) where R1 means (a) ; X1 means H or F; X12 means H or F; Q1 means (b) ; Z2 means -N(R7)-, -O-; R7 means R3-O-C(O)- where R3 is phenyl; m = 1; n1 = 0, 1 or 2; n2 = 0, 1 or 2; n3 = 5-(n1 + n2). EFFECT: new method of synthesis of 5-hydroxy- -methyl-substituted oxazolidinones, 5-aminomethyl-substituted oxazolidinone amines, new derivatives of oxazolidinone sulfonate. 18 cl, 4 dwg, 24 ex

7. 发明专利

DE69738457T2 未知
公开(公告)号：DE69738457T2
公开(公告)日：2008-12-24
申请号：DE69738457
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： A 5-aminomethyl-substituted oxalidine amide is prepared by reacting a 5-hydroxymethyl-substituted oxazolidinone alcohol with a sulfonylating agent, and reacting the resultant oxazolidinone sulfonate ammonia. The sulfonates are new conpounds.

8. 发明专利

AT383347T 未知
公开(公告)号：AT383347T
公开(公告)日：2008-01-15
申请号：AT01302264
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： A 5-aminomethyl-substituted oxalidine amide is prepared by reacting a 5-hydroxymethyl-substituted oxazolidinone alcohol with a sulfonylating agent, and reacting the resultant oxazolidinone sulfonate ammonia. The sulfonates are new conpounds.

9. 发明专利

CA2243706C AZOLYL PIPERAZINYL PHENYL OXAZOLIDINONE ANTIMICROBIALS 未知
公开(公告)号：CA2243706C
公开(公告)日：2005-10-04
申请号：CA2243706
申请日：1997-02-18
申请人： PHARMACIA & UPJOHN CO LLC
发明人： VAILLANCOURT VALERIE A , SMITH HERMAN W , GADWOOD ROBERT C , TOOPS DANA S , BARBACHYN MICHAEL R
IPC分类号： A61K31/495 , C07D263/24 , C07D263/58 , C07D413/12 , C07D417/12 , C07D419/12
摘要： Compounds useful in the preparation of pharmaceutical preparations for the treatment of microbial infection where such compounds are of structural formula (I) or pharmaceutically acceptable salts thereof wherein: R1 is -CHO, -COCH3, - COCHCl2, -COCHF2, -CO2CH3, -SO2CH3, or -COCH2OH; X1 and X2 are independently H, F, or Cl; and Q is a five-membered ring heterocycle (azolyl ring) of general form (a) wherein A, B, and C, are independently oxygen (O), nitrogen (N), sulfur (S) or carbon (C). In all cases, the piperazine nitrogen atom is attached at the carbon atom of the carbon-nitrogen double bond.

10. 发明专利

DK1114819T3 未知
公开(公告)号：DK1114819T3
公开(公告)日：2008-04-14
申请号：DK01302264
申请日：1997-03-28
申请人： PHARMACIA & UPJOHN CO LLC
发明人： PEARLMAN BRUCE A , PERRAULT WILLIAM R , BARBACHYN MICHAEL R , MANNINEN PETER R , TOOPS DANA S , HOUSER DAVID J , FLECK THOMAS J
IPC分类号： C07D263/24 , C07D263/20 , C07D295/00 , C07D413/04 , C07D413/10 , C07D487/04 , C07D521/00
摘要： A 5-aminomethyl-substituted oxalidine amide is prepared by reacting a 5-hydroxymethyl-substituted oxazolidinone alcohol with a sulfonylating agent, and reacting the resultant oxazolidinone sulfonate ammonia. The sulfonates are new conpounds.

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