GB962797A - Steroid-21-amino-acid esters and process for their manufacture - Google Patents

Steroid-21-amino-acid esters and process for their manufacture

Info

Publication number
GB962797A
GB962797A GB3910760A GB3910760A GB962797A GB 962797 A GB962797 A GB 962797A GB 3910760 A GB3910760 A GB 3910760A GB 3910760 A GB3910760 A GB 3910760A GB 962797 A GB962797 A GB 962797A
Authority
GB
United Kingdom
Prior art keywords
prednisolone
methyl
lower alkyl
hydrogen
mesyl
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
GB3910760A
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.)
Hoechst AG
Original Assignee
Hoechst AG
Farbwerke Hoechst 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 Hoechst AG, Farbwerke Hoechst AG filed Critical Hoechst AG
Publication of GB962797A publication Critical patent/GB962797A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)

Abstract

The invention comprises steroids of the formula: <FORM:0962797/C1/1> (wherein n is zero, 1 or 2, R is hydrogen, lower alkyl, phenyl or methoxy-phenyl, R1 is hydrogen or lower alkyl, and R2 and R3 are each hydrogen or lower alkyl or R2 and R3 together with the nitrogen atom form a saturated, 5- or 6-membered heterocyclic ring which may be interrupted by an oxygen atom; "lower alkyl" referring to alkyl groups of 1 to 4 carbon atoms) and acid-addition salts thereof; and their preparation by reacting 21-chloro- or 21-mesyl-6a -methyl-prednisolone with an alkali metal salt of the appropriate amino-acid in the presence of a dialkyl-formamide. Examples are given. 21-Mesyl-6a -methyl-prednisolone is prepared by reacting 6a -methyl-prednisolone with methane sulphonyl chloride in pyridine at 0 DEG C. 21-Chloro-6a -methyl-prednisolone is prepared from the same reactants in acetone and pyridine at reflux temperature. The prednisolone derivatives of the invention, which are stated to have glucocorticoidal and anti-inflammatory activity, may be made up into pharmaceutical compositions with suitable carriers. Specification 879,208 is referred to.
GB3910760A 1959-11-14 1960-11-14 Steroid-21-amino-acid esters and process for their manufacture Expired GB962797A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DEF29851A DE1126386B (en) 1959-11-14 1959-11-14 Process for the preparation of steroid 21-amino acid esters

Publications (1)

Publication Number Publication Date
GB962797A true GB962797A (en) 1964-07-01

Family

ID=7093490

Family Applications (1)

Application Number Title Priority Date Filing Date
GB3910760A Expired GB962797A (en) 1959-11-14 1960-11-14 Steroid-21-amino-acid esters and process for their manufacture

Country Status (3)

Country Link
CH (1) CH391698A (en)
DE (1) DE1126386B (en)
GB (1) GB962797A (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4443440A (en) * 1982-08-30 1984-04-17 The Upjohn Company Amine containing ester prodrugs of corticosteroids
US4456602A (en) * 1982-08-23 1984-06-26 The Upjohn Company Amine containing ester prodrugs of corticosteroids
FR2600653A1 (en) * 1986-06-24 1987-12-31 Pasteur Strasbourg Universite COMPOUNDS OF ASSOCIATIVE SYNTHESIS OF SULFUR OR NON-SULFUR AMINE ACIDS WITH D-4 PREGNENE 3,20-DIONE DERIVATIVES OR WITH D-1,4 PREGNADIENE 3,20-DIONE DERIVATIVES WITH GLUCOCORTICOID AND ANTI-INFLAMMATORY PROPERTIES, PROCESSES OF OBTAINING, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. PHARMACOLOGICAL PROPERTIES AND APPLICATIONS
EP0351561A1 (en) * 1988-06-28 1990-01-24 Kabi Pharmacia AB Novel esters of estramustine

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB819170A (en) * 1955-02-03 1959-08-26 Pfizer & Co C Steroid compounds and the preparation thereof

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4456602A (en) * 1982-08-23 1984-06-26 The Upjohn Company Amine containing ester prodrugs of corticosteroids
US4443440A (en) * 1982-08-30 1984-04-17 The Upjohn Company Amine containing ester prodrugs of corticosteroids
FR2600653A1 (en) * 1986-06-24 1987-12-31 Pasteur Strasbourg Universite COMPOUNDS OF ASSOCIATIVE SYNTHESIS OF SULFUR OR NON-SULFUR AMINE ACIDS WITH D-4 PREGNENE 3,20-DIONE DERIVATIVES OR WITH D-1,4 PREGNADIENE 3,20-DIONE DERIVATIVES WITH GLUCOCORTICOID AND ANTI-INFLAMMATORY PROPERTIES, PROCESSES OF OBTAINING, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. PHARMACOLOGICAL PROPERTIES AND APPLICATIONS
WO1988000202A1 (en) * 1986-06-24 1988-01-14 Universite Louis Pasteur De Strasbourg Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives
EP0254655A1 (en) * 1986-06-24 1988-01-27 Université Louis Pasteur de Strasbourg Etablissement public à caractère scientifique et culturel Associated synthesis compounds from sulfurized or non-sulfurized amino acids with pregnane derivatives, their preparation and their use
US4913852A (en) * 1986-06-24 1990-04-03 Catherine Milioni Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives
EP0351561A1 (en) * 1988-06-28 1990-01-24 Kabi Pharmacia AB Novel esters of estramustine
US5036062A (en) * 1988-06-28 1991-07-30 Pharmacia Ab Novel esters
LT3548B (en) 1988-06-28 1995-11-27 Kabi Pharmacia Ab Novel esters, method for the preparation thereof and pharmaceutical composition

Also Published As

Publication number Publication date
CH391698A (en) 1965-05-15
DE1126386B (en) 1962-03-29

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