C07J1/0074

INTERMEDIATE FOR PREPARING FULVESTRANT AND PREPARATION METHOD THEREFOR
20250122236 · 2025-04-17 ·

The invention relates to a fulvestrant intermediate and a preparation method thereof. Specifically, the invention relates to a compound shown as a formula V and a preparation method thereof, and R.sup.1 is hydrogen or a hydroxyl protecting group. The invention also relates to a preparation method for the synthesis of fulvestrant from the compound as shown in the formula V. The method has the advantages of short reaction steps, mild and safe reaction conditions, high selectivity, simplicity and convenience in operation and purification, high synthesis efficiency and the like, and is suitable for large-scale production.

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PROCESS FOR THE PREPARATION OF TRENBOLONE ACETATE HAVING A DEFINITE PARTICLE SIZE DISTRIBUTION AND A IRREGULAR HEXAGON PLATES CRYSTAL HABIT

Object of the present invention is an improved process for the preparation of Trenbolone Acetate of formula (I) having irregular hexagon plates crystal habit and/or a median value (D50) of the particle size distribution comprised in the range from 50 m to 80 m, or from 60 m to 90 m, or from 90 m to 250 m, by means of a crystallization wherein an addition of a seed having a median value (D50) of the particle size distribution comprised respectively in the range from 8 m to 15 m, or from 15 m to 20 m, or from 20 m to 90 m, to a solution of Trenbolone Acetate in a solvent, wherein the solvent is a C2-C5 alkyl alcohol or mixture thereof.

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19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):

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and pharmaceutically acceptable salts thereof; wherein custom-character, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Process for the preparation of trenbolone and/or trenbolone acetate

Object of the present invention is an improved process for the preparation of Trenbolone (I-b) and/or Trenbolone Acetate (I-a) comprising the reaction of the compound of formula (II): wherein R is H or Ac; with an oxidant agent in presence of an acid. ##STR00001##

2-methoxyestradiol derivatives and medical uses thereof

The present invention relates to novel 2-Methoxyestradiol derivatives and their medical use. In particular, the novel derivatives of the present invention are useful for the treatment or prevention of liver or lung fibrosis. Accordingly, the present invention also provides medical uses of the 2-Methoxyestradiol derivatives of the present invention. The present invention also provides a method of treating or preventing liver or lung fibrosis comprising administering an effective amount of the 2-Methoxyestradiol derivatives of the present invention.