Patent classifications
C07J15/005
METHODS FOR IMPROVED PRODUCTION OF VITAMINS D2 AND D3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.
IRRADIATION PROCESS OF PRO VITAMIN D
The invention discloses an improved process for production of vitamin D3 from 7-dehydrocholesterol (7-DHC) and to a simple process for recovery unreacted 7-DHC for further reuse. The invention further describes a process for isolation and purification of Vitamin D3.
Methods for improved production of vitamins D.SUB.2 .and D.SUB.3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.
Process for the preparation of 9 beta,10 alpha-progesterone (retroprogesterone)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below. ##STR00001##
PROCESS FOR THE PREPARATION OF 9 BETA,10 ALPHA-PROGESTERONE (RETROPROGESTERONE)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below.
##STR00001##
COMPOSITIONS AND METHODS OF TREATING CONDITIONS
The present disclosure provides for pharmaceutical composition and methods of treating a condition using the pharmaceutical composition. The condition to be treated in a subject in need of treatment can include an infection or non-viral hyper-inflammation/immune hyperactivation condition. The infection can be a coronavirus infection, HIV infection, influenza infection, or the like, where a direct or indirect result of the infection can be respiratory distress, oxidative stress, and the like that can lead to acute respiratory distress syndrome (ARDS) and/or organ dysfunction or failure.
METHODS FOR IMPROVED PRODUCTION OF VITAMINS D2 AND D3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.
Methods for improved production of vitamins D2 and D3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.
ANDROGEN RECEPTOR MODULATORS
The present disclosure relates to polycyclic (e.g., tetracyclic) androgen receptor (AR) modulators, synthetic methods for preparing such AR modulators, and methods of using such AR modulators to treat an androgen-dependent condition, such as prostate cancer or BPH. Exemplary compounds have quaternary centers at C10 and C13 and a fused cyclic ring comprising C14 and C15.
STEREOSELECTIVE C9-C10 BOND FORMATION
The present disclosure relates to synthetic methods for preparing a 9-alpha-substituted or a 9-beta-substituted steroid-like compound. In particular, the disclosure relates to methods for generating a steroidal C9-C10 bond and establishing stereochemistry at C9 in such compounds. The methods provide high levels of stereoselection in the C9-C10 bond forming process. Compounds synthesized by such methods can be used as nuclear hormone receptor modulators.