ES255441A1 - Procedure for the preparation of 16-methylene-steroids (Machine-translation by Google Translate, not legally binding) - Google Patents

Procedure for the preparation of 16-methylene-steroids (Machine-translation by Google Translate, not legally binding)

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Publication number
ES255441A1
ES255441A1 ES0255441A ES255441A ES255441A1 ES 255441 A1 ES255441 A1 ES 255441A1 ES 0255441 A ES0255441 A ES 0255441A ES 255441 A ES255441 A ES 255441A ES 255441 A1 ES255441 A1 ES 255441A1
Authority
ES
Spain
Prior art keywords
formula
methylene
steroids
17alpha
formation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
ES0255441A
Other languages
Spanish (es)
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck KGaA
Original Assignee
E Merck AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by E Merck AG filed Critical E Merck AG
Publication of ES255441A1 publication Critical patent/ES255441A1/en
Expired legal-status Critical Current

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Abstract

Process for the preparation of 16-methylene steroids of the formula A ** (See formula) ** Z = H o well OR1 R1 = H or acyl X = H o well F and its 1-dehydro derivatives, characterized in that it is treated with an epoxidizing agent 16-methyl-5,16-pregnadien-3 beta-ol-20-one or its 3-acylate and in the 16alpha, 17alpha- oxide-steroid II thus prepared, in the order of succession that is desired, a) the 16beta-methyl-16alpha, 17alpha-oxide group is dissociated by treatment with acid, with formation of a 16-methylene group and a 17alpha-OH group, b) the 3beta-OR1-5-ene system is transformed by standard methods into the 3-keto-4-ene system, c) a hydroxyl group is introduced in position 11, by incubation with hydroxylating microorganisms, d) In order to prepare the corresponding steroids with an oxygen function in position 21, the substituent Z = H is replaced by consecutive treatment with elemental bromine or alkaline solution of iodine and alkaline acylate, by the radical Z = O-acyl, and e) In order to prepare the corresponding 1-dehydro-derivatives, the saturated 1,2-bond is transformed, by treatment with ordinary dehydration agents, chemical or microbiological, in a double bond 1,2 with formation of a compound of formula B ** (See formula) ** in which X and R1 have the meaning indicated above and another double bond may exist in position 1,2, and by the fact that, when a 16-methylene steroid of the formula A in which X = F is to be prepared, a fluorine atom in the 9alpha position is introduced into the compound B by standard methods, with formation of a compound of formula C ** (See formula) ** in which Z has the meaning indicated above and another double bond may exist in position 1,2. (Machine-translation by Google Translate, not legally binding)
ES0255441A 1959-01-31 1960-01-30 Procedure for the preparation of 16-methylene-steroids (Machine-translation by Google Translate, not legally binding) Expired ES255441A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE255441X 1959-01-31

Publications (1)

Publication Number Publication Date
ES255441A1 true ES255441A1 (en) 1960-04-16

Family

ID=38567653

Family Applications (1)

Application Number Title Priority Date Filing Date
ES0255441A Expired ES255441A1 (en) 1959-01-31 1960-01-30 Procedure for the preparation of 16-methylene-steroids (Machine-translation by Google Translate, not legally binding)

Country Status (1)

Country Link
ES (1) ES255441A1 (en)

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