公开(公告)号：WO1995017404A1

公开(公告)日：1995-06-29

申请号：PCT/US1994014857

申请日：1994-12-22

Applicant: ALLIEDSIGNAL, INC.

Inventor： ALLIEDSIGNAL, INC. ,  POSS, Andrew, Joseph ,  SHIA, George

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: The present invention relates to the preparation and uses of 1-substitued-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts, specifically 1-hydroxyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts as reagents for the introduction of fluorine in organic compounds. In formula (I) Z is OH, OR, OC(O)R, SO3, SO3, SO2R, NO2, NO, or P(O) (OR)2 with R being an aryl or C1-C8 alkyl, where n represents 0, 1 or 2; each R1, R2, R3, R4 and R5 independently represents hydrogen, C1-C8 alkyl, aryl, C1-C8 alkyl; and each X independently represents a counterion or 2X represents a single divalent counterion.

Abstract translation: 本发明涉及1-取代-4-氟-1,4-二氮鎓双环[2.2.2]辛烷盐，特别是1-羟基-4-氟-1,4-二氮鎓双环[2.2.2]辛烷的制备和用途， 辛烷盐作为在有机化合物中引入氟的试剂。 在式（I）中，Z是OH，OR，OC（O）R，SO 3，SO 3，SO 2 R，NO 2，NO或P（O）（OR）2，其中R是芳基或C 1 -C 8烷基， 0，1或2; 每个R 1，R 2，R 3，R 4和R 5独立地表示氢，C 1 -C 8烷基，芳基，C 1 -C 8烷基; 并且每个X独立地表示抗衡离子，或2X - 表示单个二价的抗衡离子。

公开(公告)号：WO1997042193A1

公开(公告)日：1997-11-13

申请号：PCT/US1997007717

申请日：1997-05-06

Applicant: ALLIEDSIGNAL INC.

Inventor： ALLIEDSIGNAL INC. ,  POSS, Andrew, Joseph ,  SHIA, George, Anthony ,  LAVERY, Dennis, Michael

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having formula (I) wherein the Z substituent is OH, OR, OC(O)R, SO3, SO2R, NO2, NO, or PO(OR)2, wherein R is an aryl or C1-C8 alkyl group; n is 0, 1 or 2; each of R1, R2, R3, R4 and R5 independently represent hydrogen, C1 to C8 alkyl, or aryl. 1-substituted-1,4-diazoniabicyclo[2.2.2]octane or 1,4-diazoniabicyclo[2.2.2]octane mono-N-oxide is reacted to attach the Z group and then the result is reacted with molecular fluorine in the presence of a solvent that substantially does not react with fluorine and a fluoride scavenger that results in an X counter ion. These compounds are useful as fluorinating agents for the introduction of fluorine into organic compounds.

Abstract translation: 具有式（I）的1-取代-4-氟-1,4-二氮鎓双环[2.2.2]辛烷盐的方法，其中Z取代基是OH，OR，OC（O）R，SO 3，SO 2 R，NO 2， NO或PO（OR）2，其中R是芳基或C 1 -C 8烷基; n为0,1或2; R 1，R 2，R 3，R 4和R 5各自独立地表示氢，C 1至C 8烷基或芳基。 1-取代-1,4-二氮鎓二环[2.2.2]辛烷或1,4-二氮鎓双环[2.2.2]辛烷单-N-氧化物反应以附着Z基团，然后结果与分子氟反应 基本上不与氟反应的溶剂的存在和导致X抗衡离子的氟化物清除剂。 这些化合物可用作将氟引入有机化合物中的氟化剂。

公开(公告)号：WO1997032907A2

公开(公告)日：1997-09-12

申请号：PCT/US1997003270

申请日：1997-03-05

Applicant: ALLIEDSIGNAL INC.

Inventor： ALLIEDSIGNAL INC. ,  VAN DER PUY, Michael ,  MCKOWN, Jeffrey, Warren ,  PHAM, Hang, Thanh ,  POSS, Andrew, Joseph ,  SINGH, Rajiv, Ratna

IPC: C08F08/20

CPC classification number: C08F8/20

Abstract: Fluorination processes using hydrogen fluoride-containing fluorinating agents that are safely and easily handled, transported, and stored and that also exhibit good reactivity are provided. More particularly, the invention provides processes for producing fluorinated products using fluorinating agents comprising hydrogen fluoride and a carrier that may be an acid salt or a water-soluble polymer.

Abstract translation: 提供使用含氟化氢的氟化剂的氟化方法，其安全且容易地处理，运输和储存并且还表现出良好的反应性。 更具体地说，本发明提供使用包含氟化氢和可以是酸性盐或水溶性聚合物的载体的氟化剂来生产氟化产物的方法。

公开(公告)号：WO1996008502A1

公开(公告)日：1996-03-21

申请号：PCT/US1995011098

申请日：1995-09-05

Applicant: ALLIEDSIGNAL INC.

Inventor： ALLIEDSIGNAL INC. ,  POSS, Andrew, Joseph ,  SHIA, George, Anthony

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: (8S)-8-fluoroerythromycins are prepared by reacting 8,9-anhydroerythromycin 6,9-hemiacetals or an N-oxide thereof with a carboxylic acid and an N-F fluorinating agent. The anhydro starting material may be prepared in situ from erythromycins or an N-oxide derivative thereof. The (8S)-8-fluoroerythromycin products are useful antibacterial agents.

Abstract translation: （8S）-8-氟尿嘧啶通过使8,9-脱水红霉素6,9-半缩醛或其N-氧化物与羧酸和N-F氟化剂反应来制备。 脱水原料可以从红霉素或其N-氧化物衍生物原位制备。 （8S）-8-氟红霉素产品是有用的抗菌剂。

公开(公告)号：EP0741730A1

公开(公告)日：1996-11-13

申请号：EP95906105.0

申请日：1994-12-22

Applicant: AlliedSignal Inc.

Inventor： POSS, Andrew, Joseph ,  SHIA, George

IPC: C07D487

CPC classification number: C07D487/08

Abstract: The present invention relates to the preparation and uses of 1-substitued-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts, specifically 1-hydroxyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts as reagents for the introduction of fluorine in organic compounds. In formula (I) Z is OH, OR, OC(O)R, SO3, SO3, SO2R, NO2, NO, or P(O) (OR)2 with R being an aryl or C1-C8 alkyl, where n represents 0, 1 or 2; each R1, R2, R3, R4 and R5 independently represents hydrogen, C1-C8 alkyl, aryl, C1-C8 alkyl; and each X- independently represents a counterion or 2X- represents a single divalent counterion.

公开(公告)号：EP0741730B1

公开(公告)日：1999-10-06

申请号：EP95906105.2

申请日：1994-12-22

Applicant: AlliedSignal Inc.

Inventor： POSS, Andrew, Joseph ,  SHIA, George

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: The present invention relates to the preparation and uses of 1-substitued-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts, specifically 1-hydroxyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts as reagents for the introduction of fluorine in organic compounds. In formula (I) Z is OH, OR, OC(O)R, SO3, SO3, SO2R, NO2, NO, or P(O) (OR)2 with R being an aryl or C1-C8 alkyl, where n represents 0, 1 or 2; each R1, R2, R3, R4 and R5 independently represents hydrogen, C1-C8 alkyl, aryl, C1-C8 alkyl; and each X- independently represents a counterion or 2X- represents a single divalent counterion.

公开(公告)号：EP0665831B1

公开(公告)日：1997-03-19

申请号：EP93923958.8

申请日：1993-10-20

Applicant: AlliedSignal Inc.

Inventor： WAGNER, William, Joseph ,  SHIA, George, Anthony ,  POSS, Andrew, Joseph

IPC: C07C303/40 ,  C07C311/48 ,  C07D285/00

CPC classification number: C07D285/01 ,  C07C303/40 ,  C07C311/48

Abstract: The present invention relates to a process of preparing N-benzenesulfonimides comprising reacting an alkali metal salt of a sulfonimide with fluorine in the presence of water or water/organic solvent mixtures. N-fluorosulfonimides are useful as fluorinating agents. The N-fluorosulfonimides allow the introduction of fluorine into organic compounds under mild conditions.

公开(公告)号：EP0885249A2

公开(公告)日：1998-12-23

申请号：EP97908816.0

申请日：1997-03-05

Applicant: AlliedSignal Inc.

Inventor： VAN DER PUY, Michael ,  MCKOWN, Jeffrey, Warren ,  PHAM, Hang, Thanh ,  POSS, Andrew, Joseph ,  SINGH, Rajiv, Ratna

IPC: C08F8

CPC classification number: C08F8/20

Abstract: Fluorination processes using hydrogen fluoride-containing fluorinating agents that are safely and easily handled, transported, and stored and that also exhibit good reactivity are provided. More particularly, the invention provides processes for producing fluorinated products using fluorinating agents comprising hydrogen fluoride and a carrier that may be an acid salt or a water-soluble polymer.

公开(公告)号：EP0842177A1

公开(公告)日：1998-05-20

申请号：EP97922706.0

申请日：1997-05-06

Applicant: AlliedSignal Inc.

Inventor： POSS, Andrew, Joseph ,  SHIA, George, Anthony ,  LAVERY, Dennis, Michael

IPC: C07D487

CPC classification number: C07D487/08

Abstract: A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having formula (I) wherein the Z substituent is OH, OR, OC(O)R, SO3, SO2R, NO2, NO, or PO(OR)2, wherein R is an aryl or C1-C8 alkyl group; n is 0, 1 or 2; each of R1, R2, R3, R4 and R5 independently represent hydrogen, C1 to C8 alkyl, or aryl. 1-substituted-1,4-diazoniabicyclo[2.2.2]octane or 1,4-diazoniabicyclo[2.2.2]octane mono-N-oxide is reacted to attach the Z group and then the result is reacted with molecular fluorine in the presence of a solvent that substantially does not react with fluorine and a fluoride scavenger that results in an X counter ion. These compounds are useful as fluorinating agents for the introduction of fluorine into organic compounds.

公开(公告)号：EP0665831A1

公开(公告)日：1995-08-09

申请号：EP93923958.0

申请日：1993-10-20

Applicant: AlliedSignal Inc.

Inventor： WAGNER, William, Joseph ,  SHIA, George, Anthony ,  POSS, Andrew, Joseph

IPC: C07D285 ,  C07C303 ,  C07C311

CPC classification number: C07D285/01 ,  C07C303/40 ,  C07C311/48

Abstract: The present invention relates to a process of preparing N-benzenesulfonimides comprising reacting an alkali metal salt of a sulfonimide with fluorine in the presence of water or water/organic solvent mixtures. N-fluorosulfonimides are useful as fluorinating agents. The N-fluorosulfonimides allow the introduction of fluorine into organic compounds under mild conditions.