WO2026133170 - INTERMEDIATES OF ELACESTRANT AND METHODS OF MAKING AND USING THE SAME
National phase entry is expected:
Publication Number
WO/2026/133170
Publication Date
25.06.2026
International Application No.
PCT/IB2025/063019
International Filing Date
16.12.2025
Title **
[English]
INTERMEDIATES OF ELACESTRANT AND METHODS OF MAKING AND USING THE SAME
[French]
INTERMÉDIAIRES D'ÉLACESTRANT ET LEURS PROCÉDÉS DE FABRICATION ET D'UTILISATION
Applicants **
BERLIN-CHEMIE AG
Inventors
MORINI, Francesca
MASI, Matteo
RAMACCIOTTI, Alessio
D’ARATA, Fabio
CALVANI, Federico
BONACCORSI, Fabrizio
Priority Data
102024000029406
20.12.2024
IT
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Abstract[English]
The present disclosure relates to novel intermediates in the synthesis of elacestrant and methods of making the same. The chiral compound N-(2-((1R,2S)-6-(benzyloxy)-1-hydroxy-1,2,3,4- tetrahydronaphthalen-2-yl)-5-methoxyphenyl)acetamide (Compound (I-1)), is prepared in two steps: (1) a Pd-catalyzed α-arylation of a ketone precursor, 6-(benzyloxy)-3,4-dihydronaphthalen- 1(2H)-one, (Compound (a-1)), with N-(2-bromo-5-methoxyphenyl)acetamide (Compound (b- 1)); and (2) the asymmetric transfer hydrogenation of the product from Step 1, N-(2-(6- (benzyloxy)-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)-5-methoxyphenyl)acetamide (Compound (c-1)), to produce N-(2-((1R,2S)-6-(benzyloxy)-1-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)-5- methoxyphenyl)acetamide (Compound (I-1)). The chiral compound (R)-6-(2-amino-4- methoxyphenyl)-5,6,7,8-tetrahydronaphtalen-2-ol (Compound (d)) is produced from Compound (I-1) by two additional steps: 3) dehydroxylation and debenzylation of N-(2-((1R,2S)-6- (benzyloxy)-1-hydroxy-1,2,3,4-tetrahydronaphtalen-2-yl)-5-methoxyphenyl)acetamide (Compound (I-1)) to produce N-(2-(6-hydroxy)-1,2,3,4-tetrahydronaphtalen-2-yl)-5- methoxyphenyl)acetamide (Compound (III-1)); and 4) hydrolysis of N-(2-(6-hydroxy)-1,2,3,4- tetrahydronaphtalen-2-yl)-5-methoxyphenyl)acetamide (Compound (III-1)) to produce (R)-6-(2- amino-4-methoxyphenyl)-5,6,7,8-tetrahydronaphtalen-2-ol (Compound (d)).[French]
La présente divulgation concerne de nouveaux intermédiaires dans la synthèse de l'élacestrant et leurs procédés de fabrication. Le composé chiral N-(2-((1R,2S)-6-(benzyloxy)-1-hydroxy-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (I-1)), est préparé en deux étapes : (1) une α-arylation catalysée par Pd d'un précurseur de cétone, 6-(benzyloxy)-3,4-dihydronaphtalén-1(2H)-one, (composé (a-1)), avec du N-(2-bromo-5-méthoxyphényl)acétamide (composé (b-1)) ; et (2) l'hydrogénation par transfert asymétrique du produit de l'étape 1, N-(2-(6-(benzyloxy)-1-oxo-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (c-1)), pour produire du N-(2-((1R,2S)-6-(benzyloxy)-1-hydroxy-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (I-1)). Le composé chiral (R)-6-(2-amino-4-méthoxyphényl)-5,6,7,8-tétrahydronaphtalén-2-ol (composé (d)) est produit à partir du composé (I-1) par deux étapes supplémentaires : 3) déshydroxylation et débenzylation de N-(2-((1R,2S)-6-(benzyloxy)-1-hydroxy-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (I-1)) pour produire du N-(2-(6-hydroxy)-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (III-1)) ; et 4) hydrolyse de N-(2- (6-hydroxy)-1,2,3,4-tétrahydronaphtalén-2-yl)-5-méthoxyphényl)acétamide (composé (III-1)) pour produire du (R)-6-(2-amino-4-méthoxyphényl)-5,6,7,8-tétrahydronaphtalén-2-ol (composé (d)).