公开(公告)号：JP2003261546A

公开(公告)日：2003-09-19

申请号：JP2002355604

申请日：2002-12-06

Applicant: BASF AG

Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  MOHRY ANDRE

IPC: C07D213/66 ,  B01D3/14 ,  B01J14/00 ,  C07D213/67 ,  C07D263/42

Abstract: PROBLEM TO BE SOLVED: To provide a new process for the continuous preparation of a 5- alkoxy-substituted oxazole in high yield and high space-time yield. SOLUTION: The process for the continuous preparation of a 5-alkoxy- substituted oxazole of formula I (R 1 is a substituted or unsubstituted 1-6C alkyl; and R 2 is H or a substituted or unsubstituted 1-6C alkyl) comprises the conversion of a continuously charged α-isocyanoalkanoic acid ester of formula II to the 5-alkoxy-substituted oxazole of formula I in a reactor at ≥80°C in the presence of an assistant selected from continuously charged alcohols and esters and the continuous discharge of the reaction product from the reactor. COPYRIGHT: (C)2003,JPO

公开(公告)号：JP2003201283A

公开(公告)日：2003-07-18

申请号：JP2002227742

申请日：2002-08-05

Applicant: BASF AG

Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  MOHRY ANDRE

IPC: C07D213/67 ,  C07D263/42

Abstract: PROBLEM TO BE SOLVED: To provide a method for continuously producing a 5-alkoxy-substituted oxazole and a method for producing a pyridoxine derivative by using the same. SOLUTION: This method for obtaining a pyridoxine derivative is provided by converting an α-isocyanoalkanoic acid ester expressed by the formula II in the presence of continuously supplied base at ≥80°C temperature to a 5- alkoxy-substituted oxazole I, taking it out from a reactor at the same time with the reaction, performing a reaction of the compound I with a compound VI to make a compound VII, and acid-treating it to obtain a pyridoxine derivative IX (in formulae, R 1 is an alkyl, R 2 is H or an alkyl, R 3 , R 4 are each independently a protection group of hydroxy group). COPYRIGHT: (C)2003,JPO

公开(公告)号：AT384706T

公开(公告)日：2008-02-15

申请号：AT02016707

申请日：2002-07-26

Applicant: BASF AG

Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  MOHRY ANDRE

IPC: C07D263/42

Abstract: Continuous production of 5-alkoxy oxazoles (I) comprises heating an alkyl alpha -isocyanoalkanoate ester (II) at a temperature above 80 degrees C in the presence of an auxiliary agent and withdrawing the product from the reactor. Continuous production of 5-alkoxy oxazoles of formula (I) comprises heating an alkyl alpha -isocyanoalkanoate ester of formula (II) at a temperature above 80 degrees C in the presence of an auxiliary agent and withdrawing the product from the reactor. R1 = optionally substituted 1-6C alkyl; R2 = H or optionally substituted 1-6C alkyl. An Independent claim is also included for a process for producing pyridoxine derivatives of formula (IX), comprising: (1) converting an amino acid of formula (III) to an ester of formula (IV); (2) converting (IV) to a formamido ester of formula (IV); (3) converting (IV) to (II); (4) converting (II) to (I) as above; (5) reacting (I) with a protected diol of formula (VI) to form a Diels-Alder adduct of formula (VII); and (6) converting (VII) to (IX) by acid treatment and deprotection. R3, R4 = protecting groups or together form a protecting group.

公开(公告)号：DE10137627A1

公开(公告)日：2003-02-20

申请号：DE10137627

申请日：2001-08-03

Applicant: BASF AG

Inventor： RUST HARALD ,  BURKART KIRSTEN ,  FAUST TILLMANN ,  HENKELMANN JOCHEM ,  KINDLER ALOIS ,  KNOLL CHRISTIAN ,  MOHRY ANDRE

IPC: C07D213/67 ,  C07D263/42 ,  C07D213/66

Abstract: Continuous production of 5-alkoxy oxazoles (I) comprises heating an alkyl alpha -isocyanoalkanoate ester (II) at a temperature above 80 deg C in the presence of an auxiliary agent and withdrawing the product from the reactor. Continuous production of 5-alkoxy oxazoles of formula (I) comprises heating an alkyl alpha -isocyanoalkanoate ester of formula (II) at a temperature above 80 deg C in the presence of an auxiliary agent and withdrawing the product from the reactor. R1 = optionally substituted 1-6C alkyl; R2 = H or optionally substituted 1-6C alkyl. An Independent claim is also included for a process for producing pyridoxine derivatives of formula (IX), comprising: (1) converting an amino acid of formula (III) to an ester of formula (IV); (2) converting (IV) to a formamido ester of formula (IV); (3) converting (IV) to (II); (4) converting (II) to (I) as above; (5) reacting (I) with a protected diol of formula (VI) to form a Diels-Alder adduct of formula (VII); and (6) converting (VII) to (IX) by acid treatment and deprotection. R3, R4 = protecting groups or together form a protecting group.