Abstract:
:Estrogen sulfamates are promising hormones by oral administration. Therefore, generally applicable and convenient methods for the multigram synthesis of these derivatives are desirable. Numerous estra-1,3,5(10)-trienes derived from estrone, estradiol. 14 alpha,15 alpha-methylenestradiol, ethinylestradiol, and estriol have been esterified with sulfamoyl chloride and N-methylsulfamoyl chloride by a novel approach involving the use of 2,6-di-tert-butylpyridines as bases and chemoselective hydroxy group protections. These pathways circumvent the nonselective formation of esters and side reactions by in situ generated azasulfenes. For toxicological and clinical studies a new synthesis of estrone sulfamate on a 100-g scale was developed using dimethylformamide as the solvent and base.
journal_name
Steroidsjournal_title
Steroidsauthors
Schwarz S,Thieme I,Richter M,Undeutsch B,Henkel H,Elger Wdoi
10.1016/s0039-128x(96)00200-0subject
Has Abstractpub_date
1996-12-01 00:00:00pages
710-7issue
12eissn
0039-128Xissn
1878-5867pii
S0039-128X(96)00200-0journal_volume
61pub_type
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