Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

##STR00001##

Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

##STR00001##

Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia. ##STR00001##

Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

##STR00001##

Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

##STR00001##

The present invention relates to a new stereoselective process for the synthesis of 17()-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17()-17-acetyl-17-hydroxy-estr-4-en-3-one (gestonorone) is an important intermediate in the synthesis of the active ingredients having progestogen activitysuch as gestonorone capronate and nomegestroi acetate. Formulas (I), (II) and (III). ##STR00001##