METHOD FOR PRODUCING MEPREGHENOL DI-ACETATE FROM MEGESTROL ACETATE Russian patent published in 2018 - IPC C07J5/00 C07J75/00 

Abstract RU 2661155 C1

FIELD: technological processes.

SUBSTANCE: invention relates to a process for the preparation of mepreghenol di-acetate comprising the step of reducing the megestrol acetate with sodium borohydride in an alcoholic solution to obtain a steroidal alcohol (mepreghenol 17-acetate) and the reaction of its acetylation with acetic anhydride, in which the reduction step is carried out in aqueous isopropyl alcohol with a water content of 10 to 20 % in the presence of hydrochloric acid and at a temperature maintained in the range of 11±2 °C, the acetylation is carried out in acetone in the presence of a tertiary amine or a combination of tertiary amines as a catalyst, followed by precipitation of the desired product with aqueous ammonia.

EFFECT: simple and safe method for producing high-yield diacetate of mepreghenol is developed, which provides the possibility of scaling the process.

5 cl, 1 tbl, 3 ex

Similar patents RU2661155C1

Title Year Author Number
17α-ACETOXY-3β-HEXANOYLOXY-6-METHYLPREGNA-4,6-DIEN-20-ON WITH GESTAGENIC, CONTRACEPTIVE AND ANTITUMOR ACTIVITY, AND THE METHOD OF ITS OBTAINING 2018
  • Andryushina Valentina Aleksandrovna
  • Stytsenko Tatyana Semenovna
  • Karpova Natalya Viktorovna
  • Yaderets Vera Vladimirovna
  • Dzhavakhiya Vakhtang Vitalevich
  • Skryabin Konstantin Georgievich
RU2683953C1
METHOD OF PREPARATION OF 17α-ACETOXY-3β-BUTANOYLOXY-6-METHYL-PREGNA-4,6-DIEN-20-ONE FROM MEGESTROL ACETATE 2017
  • Andryushina Valentina Aleksandrovna
  • Stytsenko Tatyana Semenovna
  • Karpova Natalya Viktorovna
  • Dzhavakhiya Vakhtang Vitalevich
  • Skryabin Konstantin Georgievich
  • Shimanovskij Nikolaj Lvovich
  • Fedotcheva Tatyana Aleksandrovna
  • Semejkin Aleksandr Vladimirovich
RU2653507C1
MEDICINAL PREPARATION POSSESSING ANTITUMOR ACTIVITY 1988
  • Kadatskij G.M.
  • Grinenko G.S.
  • Korkhov V.V.
  • Nikitina G.V.
  • Dil'Man V.M.
  • Krylova N.V.
  • Stukov A.N.
  • Nevolin-Lopatin A.M.
  • Chernov V.A.
  • Sokolova A.S.
RU2039560C1
17α-ACETOXY-3β-PHENYLPROPIONYLOXY-6-METHYL-PREGNA-4,6-DIENE-20-ONE ELICITING GESTAGENOUS ACTIVITY AND MEDICINAL AGENT BASED ON THEREOF 2001
  • Tapil'Skaja N.I.
  • Korkhov V.V.
  • Grinenko G.S.
RU2200165C1
17α-ACETOXY-3β-BUTANOYLHYDROXY-6-METHYLPREGNA-4,6-DIENE-20-ONE SHOWING GESTAGENIC ACTIVITY 1996
  • Grinenko G.S.
  • Morozova L.S.
  • Korkhov V.V.
  • Lesik E.A.
  • Fadeeva N.A.
  • Kolotilov D.O.
RU2099347C1
METHOD FOR OBTAINING 6-DEHYDRO-6-METHYLHYDROCORTISONE OR ESTER THEREOF FROM HYDROCORTISONE 21-ACETATE 2017
  • Savinova Tatyana Stepanovna
  • Kazantsev Aleksej Vitalevich
  • Lukashev Nikolaj Vadimovich
RU2663893C1
METHOD FOR PRODUCING 6-METHYLENEHYDROCORTISONE OR ESTERS THEREOF FROM HYDROCORTISONE 21-ACETATE 2017
  • Savinova Tatyana Stepanovna
  • Kazantsev Aleksej Vitalevich
  • Lukashev Nikolaj Vadimovich
RU2664101C1
PRODUCTION METHOD FOR ULIPRISTAL ACETATE AND ITS INTERMEDIATES 2012
  • Luo Junzhi
  • Sun Yongqiang
  • Luo Xun
  • Yan Yimin
  • Wang Zhaojun
  • Qian Mingxia
  • Tu Yongrui
RU2624007C2
METHOD OF PREPARATION 6α-METHYLHYDROCORTISONE OR ESTERS THEREOF FROM HYDROCORTISONE 21-ACETATE 2017
  • Savinova Tatyana Stepanovna
  • Kazantsev Aleksej Vitalevich
  • Lukashev Nikolaj Vadimovich
RU2663484C1
PROCESS FOR PREPARING 21-HYDROXY-16,17ALPHA-EPIMINO-20-KETOSTREROYDS 0
  • Kamernitskij Aleksej Vladimirovich
  • Turuta Alevtina Mikhajlovna
  • Fadeeva Tatyana Mikhajlovna
SU1121267A1

RU 2 661 155 C1

Authors

Andryushina Valentina Aleksandrovna

Zejnalov Orkhan Akhmed Ogly

Dates

2018-07-12Published

2017-05-10Filed