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1. WO2017163257 - PROCESS FOR PREPARING PURE LH-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVE

Publication Number WO/2017/163257
Publication Date 28.09.2017
International Application No. PCT/IN2017/000061
International Filing Date 20.03.2017
IPC
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 29/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A61K 31/52 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
C07D 473/34 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
C07D 401/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
C07D 231/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • IND-SWIFT LABORATORIES LIMITED [IN]/[IN]
Inventors
  • ARUL, Ramakrishnan
  • SARIN, Gurdeep Singh
  • WAS, Sandeep
  • KUMAR, Vishal
Agents
  • AGGARWAL Asha
Priority Data
20161100968421.03.2016IN
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING PURE LH-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVE
(FR) PROCÉDÉ DE PRÉPARATION D’UN DÉRIVÉ LH-PYRAZOLO[3,4-D] PYRIMIDINE PUR
Abstract
(EN) The present invention relates to an efficient and industrially advantageous process for the preparation of pure lH-pyrazolo[3,4-d] pyrimidine derivative. In particular the present invention provides a process for the preparation of pure 4-amino-3-(4- phenoxyphenyl)-lH-pyrazolo[3,4-d] pyrimidine, a key intermediate of ibrutinib. Particularly, the present invention provides a process for the preparation of 3-amino-4-cyano-5-(4-phenoxy phenyl)pyrazole, wherein none of the intermediates have been isolated, an important precursor for the preparation of 4-amino-3-(4-phenoxyphenyl)- lH-pyrazolo[3,4-d] pyrimidine.
(FR) La présente invention concerne un procédé efficace et industriellement avantageux destiné à la préparation d’un dérivé 1H-pyrazolo[3,4-d] pyrimidine pur. En particulier la présente invention décrit un procédé de préparation de 4-amino-3-(4-phénoxyphényl)-1H-pyrazolo[3,4-d] pyrimidine pure, un intermédiaire clé de l’ibrutinib. En particulier, la présente invention décrit un procédé de préparation de 3-amino-4-cyano-5-(4-phénoxy phényl)pyrazole, où aucun des intermédiaires n’a été isolé, un précurseur important pour la préparation de 4-amino-3-(4-phénoxyphényl)-1H-pyrazolo[3,4-d] pyrimidine.
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