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17b Hydroxy 2a 17B Dimethyl 5a Androstan 3 One Azine

17b Hydroxy 2a 17B Dimethyl 5a Androstan 317b hydroxy 2a 17b dimethyl 5a androstan 3 one azine 18 with propylene 17 3 in order to obtain 2-(hydroxymethyl)azanaphthalene 5, the intermediate 2-(hydroxymethyl)azanaphthalen 1a is transformed into 17-hydroxy azanaphthalen-1-one 5, which in turn can be oxidized with N-chlorosuccinimide and chlorine (Cl2) into the compound of the invention 2-(azanaphthalen-1-yl-sulfonyl)propane. The synthesis of the compound according to the invention proceeds as described in the following. The synthesis reaction is divided into the stages for the preparation of the 2-(hydroxymethyl)azanaphthalen-1-one 5 starting from the 2-bromobenzaldehyde 2-bromohydroquinone 3 and ethyl cyanoacetate 4, the preparation of the ester derivative of the 1-azanaphthalene and the hydrolysis of the ester derivative to 2-(hydroxymethyl)azanaphthalen-1-one.

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What is 17b Hydroxy 2a 17b dimethyl 5a Androstan 3 One Azine?

The stage of the preparation of 2-(hydroxymethyl)azanaphthalen-1-one 5 and the stage of the preparation of the ester derivative of the 1-azanaphthalene are in particular described in Journal of the Chemical Society, Perkin Transactions, I, 1968, pages 3-15. The hydrolysis of the ester derivative of the 1-azanaphthalene into 2-(hydroxymethyl)azanaphthalen-1-one 5 in accordance with the invention is described in Applied Chem. 1972, 4 (5), pages 38-40. A method for the preparation of 2-(azanaphthalen-1-yl-sulfonyl)propane in accordance with the invention from 2-(azanaphthalen-1-yl)-methyl-sulfonate 6 and methanesulfonic acid in the presence of an inert solvent is described in European Published Patent Application No. 633,188. The 3,5-bis(trifluoromethyl)benzylidene derivative is used as an intermediate for the synthesis of the compound according to the invention.

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The synthesis reaction of the compound in accordance with the invention is divided into the stage for the preparation of the 3,5-bis(trifluoromethyl)benzylidene derivative and the stage for the preparation of the 2-(azanaphthalen-1-yl)-methyl-sulfonate. The stage of the preparation of the 3,5-bis(trifluoromethyl)benzylidene derivative is described in Acta Chemica Scandinavia, 1973, 27, pages 929-934. The stage of the preparation of the 2-(azanaphthalen-1-yl)-methyl-sulfonate is described in J.Org.Chem. 1995, 60, pages 6077-6080. The 2-(azanaphthalen-1-yl)-methyl-sulfonate is reacted in the stage with methanesulfonic acid in the presence of an inert solvent with elimination of methyl sulfite and formation of the thionylate 6, in which the compound in accordance with the invention 2-(azanaphthalen-1-yl-sulfonyl)propane is obtained as a by-product.

How is 17b Hydroxy 2a 17B Dimethyl 5a Androstan 3 One Azine Made?

The compound is purified by chromatography on silica gel or by distillation. The invention is described further in more detail with reference to examples below. The following abbreviations for the component parts of the formulas I, II and III are: The present invention also relates to a pharmaceutical composition comprising a compound of formula I, II or III, or a physiologically tolerable salts thereof, and a pharmaceutically acceptable carrier. The pharmaceutical compositions in accordance with the invention are distinguished by the fact that they show an improved efficacy against a broad spectrum of viruses. The present invention further relates to a process for preparing a pharmaceutical composition, wherein a compound of formula I, II or III, or a physiologically tolerable salts thereof, is prepared and the pharmaceutical composition is obtained by processing the compound of formula I, II or III, or a physiologically tolerable salts thereof, with a pharmaceutically acceptable carrier.

How is 17b Hydroxy 2a 17B Dimethyl 5a Androstan 3 One Azine Used For Diseases?

The present invention also relates to a process for the treatment of a disease which is ameliorated by inhibition of replication of DNA and/or inhibition of virus proliferation, or viral infection, which is characterized in that a compound of formula I, II or III, or a physiologically tolerable salts thereof, is used in a therapeutically effective amount. The use of a compound of formula I, II or III, or a physiologically tolerable salts thereof, for the manufacture of a medicament for the treatment of a disease, which is ameliorated by inhibition of replication of DNA and/or inhibition of virus proliferation, or viral infection, is thereby included.

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Furthermore, the present invention relates to the use of a compound of formula I, II or III, or a physiologically tolerable salts thereof, for the preparation of a pharmaceutical composition for the treatment of a disease which is ameliorated by inhibition of replication of DNA and/or inhibition of virus proliferation, or viral infection. In particular, the compound of formula I, II or III, or a physiologically tolerable salts thereof, may be used for the treatment of a disease which is ameliorated by inhibition of DNA or DNA-dependent RNA synthesis, and/or inhibition of virus proliferation, such as inhibition of the DNA synthesis of SV40, of the DNA synthesis of adenovirus type 5 and of the DNA synthesis of Herpesvirus type 1 (Herpes Simplex virus type 1).

These diseases are described, for example, in Current Infection Reports, 5, 1998, pages 7-10, 13, 19, 23, 25 and 30, 1999, pages 1-7, 8, 17, 19, 21, 23, 25 and 27. The present invention also relates to a method for the treatment of a disease which is ameliorated by inhibition of DNA or DNA-dependent RNA synthesis, and/or inhibition of virus proliferation, in which a compound of formula I, II or III, or a physiologically tolerable salts thereof, is administered in a therapeutically effective amount. In particular, the compound of formula I, II or III