434-22-0Relevant articles and documents
A New Synthesis of 19-Nor Steroids via 2,4-Dibromoestrogens
Numazawa, Mitsuteru,Hoshi, Kumiko,Kimura, Katsuhiko
, p. 490 - 491 (1987)
19-Nor steroids (7) and (8) have been synthesised via oxidation of 2,4-dibromoestrogens (1) and (2) with nitric acid followed by hydrogenation over palladium-on-charcoal and subsequent treatment with Nafion-H.
Where does hydrolysis of nandrolone decanoate occur in the human body after release from an oil depot?
Kalicharan,Bout,Oussoren,Vromans
, p. 721 - 728 (2016)
Long-term therapy of nandrolone (N) is recommended to increase mineral density and muscle strength. Using a parenteral sustained release drug formulation with nandrolone decanoate (ND), therapeutic N levels can be achieved and maintained. Until now, it is unknown if hydrolysis of ND into N occurs in tissue at the injection site or after systemic absorption. Therefore, hydrolysis studies were conducted to investigate the location and rate of ND hydrolysis after its release from the oil depot. ND hydrolysis was studied in porcine tissues, to mimic the human muscular and subcutaneous tissues. Additionally, the ND hydrolysis was studied in human whole blood, plasma and serum at a concentration range of 23.3–233.3?μM. ND hydrolysis only occurred in human whole blood. The hydrolysis did not start immediately, but after a lag time. The mean lag time for all studied concentrations was 34.9?±?2.5?min. Because of a slow penetration into tissue, hydrolysis of ND is found to be very low in surrounding tissue. Therefore the local generation of the active compound is clinically irrelevant. It is argued that after injection of the oil depot, ND molecules will be transported via the lymphatic system towards lymph nodes. From here, it will enter the central circulation and within half an hour it will hydrolyse to the active N compound.
SYNTHESIS OF OPTICALLY ACTIVE (+)-19-NORTESTOSTERONE BY ASYMMETRIC BIS-ANNULATION REACTION
Shimizu, Isao,Naito, Yoichiro,Tsuji, Jiro
, p. 487 - 490 (1980)
Michael reaction of 1,7-octadien-3-one with 2-methylcyclopentane-1,3-dione, followed by intramolecular aldol condensation promoted by L-amino acids produced the optically active (+)-4-(3-butenyl)-7a-methyl-5,6,7,7a-tetrahydro-indane-1,5-dione in high chem
Preparation method of [3-14C] marked 17alpha-estradiol
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Paragraph 0089; 0098-0099, (2019/06/07)
The invention belongs to the technical field of synthesis of compounds marked by radioisotope 14C, and provides a preparation method of [3-14C] marked 17alpha-estradiol. The preparation method includes the following steps that 17beta-acylated elollactone and 14C marked acetylchloride serve as starting materials, and a condensation reaction, a primary hydrolysis reaction, a Mitsunobu reaction, an aromatization reaction and a secondary hydrolysis reaction are carried out to obtain [3-14C] marked 17alpha-estradiol. The method has the advantages that the synthesis cost is low, the line is short and the product yield is high. Besides, the preparation method is easy to operate and suitable for large-scale production.
C-20 STEROID COMPOUNDS, COMPOSITIONS AND USES THEREOF TO TREAT TRAUMATIC BRAIN INJURY (TBI), INCLUDING CONCUSSIONS
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, (2016/04/09)
The present invention relates to C-20 steroid compounds, compositions and methods of use thereof to treat, minimize and/or prevent traumatic brain injury (TBI), including severe TBI, moderate TBI and mild TBI, including concussions.