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1. WO2022109481 - METHODS OF SYNTHESIZING SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS

Publication Number WO/2022/109481
Publication Date 27.05.2022
International Application No. PCT/US2021/060584
International Filing Date 23.11.2021
IPC
A61K 31/506 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
506not condensed and containing further heterocyclic rings
A61K 45/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 9/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
CPC
A61K 31/506
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
Applicants
  • ACLARIS THERAPEUTICS, INC. [US]/[US]
Inventors
  • DECRESCENZO, Gary A.
  • SPRINGER, John Robert
Agents
  • CHILDS, Carissa R.
  • FRATTINI, Gregory D.
  • STAKLEFF, Nicole N.
Priority Data
63/117,05323.11.2020US
63/239,59601.09.2021US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) METHODS OF SYNTHESIZING SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS
(FR) PROCÉDÉS DE SYNTHÈSE DE COMPOSÉS PYRIDINONE-PYRIDINYLE SUBSTITUÉS
Abstract
(EN) The present disclosure provides methods of synthesizing a compound of Formula (P)-I. The method proceeds through several different pathways including several novel chiral separations, a Sonogashira coupling, a zinc mediated reductive cyanation, as well as through various halide containing intermediates. Also disclosed is the multi-kilogram preparation of several novel intermediates.
(FR) La présente invention concerne des procédés de synthèse d'un composé de formule (P)-I. Le procédé passe à travers plusieurs voies différentes comprenant plusieurs nouvelles séparations chirales, un couplage de Sonogashira, une cyanation réductrice médiée par le zinc, ainsi que par divers intermédiaires contenant un halogénure. L'invention concerne également la préparation multi-kilogramme de plusieurs nouveaux intermédiaires.
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