WO2025210581 - A NOVEL PROCESS FOR THE PREPARATION OF (6R)-6-(2-(N-(4-(2-(ETHYLAMINO) ETHYL) BENZYL)-N-ETHYLAMINO)-4-METHOXYPHENYL)-5,6,7,8-TETRAHYDRONAPHTHALEN-2-OL DIHYDROCHLORIDE AND IT'S INTEMEDIATES

National phase entry is expected:
Publication Number WO/2025/210581
Publication Date 09.10.2025
International Application No. PCT/IB2025/053575
International Filing Date 04.04.2025
Title **
[English] A NOVEL PROCESS FOR THE PREPARATION OF (6R)-6-(2-(N-(4-(2-(ETHYLAMINO) ETHYL) BENZYL)-N-ETHYLAMINO)-4-METHOXYPHENYL)-5,6,7,8-TETRAHYDRONAPHTHALEN-2-OL DIHYDROCHLORIDE AND IT'S INTEMEDIATES
[French] NOUVEAU PROCÉDÉ DE PRÉPARATION DE DICHLORHYDRATE DE (6R)-6-(2-(N-(4-(2-(ÉTHYLAMINO)ÉTHYL)BENZYL)-N-ÉTHYLAMINO)-4-MÉTHOXYPHÉNYL)-5,6,7,8-TÉTRAHYDRONAPHTALÉN-2-OL ET SES INTERMÉDIAIRES
Applicants **
BIOPHORE INDIA PHARMACEUTICALS PVT. LTD
Inventors
PULLAGURLA, Manik Reddy
PITTA, Bhaskar Reddy
RANGISETTY, Jagadeesh Babu
Priority Data
202441027906   04.04.2024   IN
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting2100
EPO Filing, Examination, Granting12086
Japan Filing, Examination, Granting2001
South Korea Filing, Examination, Granting1805
USA Filing, Examination, Granting7740
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Total: 25,732
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Abstract[English] The present invention relates to a process for the preparation of (6R)-6-(2-(N-(4-(2- (ethylamino)ethyl)benzyl)-N-ethylamino)-4-methoxyphenyl)-5,6,7,8-tetrahydro nap- hthalen-2-ol dihydrochloride (1) and its novel intermediates thereof. Elacestrant dihydrochloride (1) The present invention further relates to a process for the preparation of intermediates of formula (3), formula (4), formula (4a), formula (5), formula (5a), formula (6), formula (6a), formula (7), formula (7a), formula (9) and formula (10). with enantiomeric excess greater than 50%.[French] La présente invention concerne un procédé de préparation de dichlorhydrate de (6R)-6-(2-(N-(4-(2-(éthylamino)éthyl)benzyl)-N-éthylamino)-4-méthoxyphényl)-5,6,7,8-tétrahydronaphthalèn-2-ol (1) et de nouveaux intermédiaires de celui-ci. La présente invention concerne en outre un procédé de préparation d'intermédiaires de formule (3), de formule (4), de formule (4a), de formule (5), de formule (5a), de formule (6), de formule (6a), de formule (7), de formule (7a), de formule (9) et de formule (10) avec un excès énantiomérique supérieur à 50%.