METHOD FOR OBTAINING A DERIVATIVE OF 7H-PYRROLO[2,3-D] PYRIMIDINE AND ITS INTERMEDIATE Russian patent published in 2021 - IPC C07D519/00 C07D487/04 C07D487/10 C07D205/04 

Abstract RU 2755618 C2

FIELD: pharmaceutics.

SUBSTANCE: presented group of inventions relates to a new compound, namely, disodium salt dihydrate of a compound [10], represented by the formula [9], or its crystalline form, demonstrating a powder X-ray diffractogram having peaks with a diffraction angle (2θ): 4.9°±0.2°, 12.3°±0.2°, 14.2°±0.2°, 14.5°±0.2°, 15.0°±0.2°, 15.5°±0.2°, 16.5°±0.2°, 18.1°±0.2°, 18.4°±0.2°, 18.6°±0.2°, 19.2°±0.2°, 20.0°±0.2°, 21.3°±0.2° or 22.7°±0.2°, 23.3°±0.2° and 24.8°±0.2°, when using CuKα-radiation. In addition, a method for obtaining disodium salt dihydrate, represented by the formula [9], is described, including the cleavage of tert-butyl from a compound of the formula [8] by processing it with acid selected from p-toluene sulfonic acid or phosphoric acid, where acid is used in amount of 1.0 to 3.0 equivalents relatively to the compound of the formula [8] and where a reaction is carried out in the presence of a solvent selected from acetonitrile, water or a mixture of these solvents; where the reaction temperature is from 40 to 60°C and where the reaction time is from 5 to 24 hours; with the subsequent formation of a compound of the formula [9] with sodium hydroxide.

EFFECT: technical result is that a new compound is obtained and described, which can be used as an intermediate compound in a method for producing a derivative of 7H-pyrrolo[2,3-d]pyrimidine, which can be used as a Janus kinase (JAK) inhibitor.

,

5 cl, 6 dwg, 8 tbl, 32 ex

Similar patents RU2755618C2

Title Year Author Number
METHOD FOR PRODUCTION OF 7H-PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AND THEIR COCRYSTALS 2017
  • Simadzaki, Takakhisa
RU2779212C2
NITROGEN-CONTAINING SPIROCYCLIC COMPOUND AND ITS APPLICATION IN MEDICINE 2010
  • Nodzi Satoru
  • Siodzaki Makoto
  • Miura Tomoya
  • Khara Esinori
  • Yamanaka Khirosi
  • Maeda Katsuya
  • Khori Akimi
  • Inoe Masafumi
  • Khase Yasunori
RU2630694C2
NOVEL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF 2005
  • Jokotani Dzuniti
  • Taniguti Joiti
  • Khara Eidzi
  • Akitsu Khitosi
  • Tada Jukie
RU2394021C2
MACROCYCLIC COMPOUND AND ITS USE 2019
  • Matsumoto, Sigemitsu
  • Khara, Rioma
  • Noguti, Naesi
  • Fukusi, Khideto
  • Niida, Ayumu
  • Sasaki, Satosi
  • Ikoma, Minoru
  • Kobayasi, Tositake
  • Maekava, Tsuesi
RU2798235C2
BICYCLIC HETEROCYCLES AS MEK KINASE INHIBITORS 2009
  • Khild Robert Ehndrju
  • Dzhekson Filip
  • Lissikatos Dzhozef
  • Prajs Stefen
  • Savi Paskal' P'Er
RU2509078C2
COMPOUND WITH METHYLLACTAM RING AND ITS USE IN PHARMACEUTICS 2019
  • Miura, Tomoya
  • Tamatani, Yoshinori
RU2809634C2
DEUTERIZED BENZIMIDAZOLE COMPOUND AND ITS MEDICAL USE 2018
  • Kanai, Toshio
  • Iwamoto, Kohei
RU2804319C2
MODULATORS OF ATP-BINDING TRANSPORTERS 2010
  • Shet Urvi
  • Fehnning Lev T. D.
  • Numa Mekhdi
  • Binch Khehjli
  • Kharli Dennis Dzhejms
  • Chzhou Tszinlan'
  • Adida Rua Sara S.
  • Khejzlvud Anna R.
  • Silina Alina
  • Vairagoundar Radzhendran
  • Van Gur Frederik F.
  • Grotenkhejs Peter Diderik Jan
  • Botfild Martin K.
RU2552353C2
PYRAZOLE COMPOUNDS SUBSTITUTED BY HETEROARYL AND THEIR APPLICATION IN PHARMACEUTICS 2019
  • Miura, Tomoya
  • Hirashima, Shintaro
  • Manabe, Tomoyuki
  • Iida, Tetsuya
  • Sakurai, Kentaro
RU2805312C2
EPOXY COMPOUND AND PRODUCTION METHOD THEREOF 2008
  • Tsubouti Khidetsugu
  • Kharaguti Josikazu
  • Khajakava Satosi
  • Utsumi Naoto
  • Taira Siniti
  • Tanada Josikhisa
  • Fudzita Nobukhisa
  • Sinkhama Koiti
  • Annaka Kimijosi
  • Furuta Takuja
RU2459822C2

RU 2 755 618 C2

Authors

Yamasaki Takakhiro

Khara Esinori

Sakaj Takayuki

Murakami Kengo

Khara Katsuesi

Manta Naoki

Dates

2021-09-17Published

2016-07-06Filed