Kali-chemie Pharma Gmbh

Akiji Asai

Peter W Thies

Samuel David

Ivan Ban

Samuell David

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes and the process for their production and the production of various intermediates are disclosed. Pharmaceutical compositions containing an effective amount of the novel compounds and a pharmaceutically acceptable carrier are also disclosed.

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group

2,9-Dioxatricyclo [4,3,1,0.sup.3,7 ] decane derivatives and

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group one of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen one of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.

2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives and pharmaceutical

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decanes and the process for their production and the production of various intermediates are disclosed. Pharmaceutical compositions containing an effective amount of the novel compounds and a pharmaceutically acceptable carrier are also disclosed.

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decanes

A process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives is disclosed, wherein a 10-methylen-3-iodomethyl compound of the formula ##STR1## is hydrogenated to obtain a mixture of the corresponding epimeric 10.beta.- and 10.alpha.-methyl-3-iodomethyl compounds, the pure 10.alpha.- and 10.beta.-methyl epimers are separated and recovered from this mixture and are reacted with a secondary amine. Optionally, the substituent in the 4-position of the resulting 10.alpha.- or 10.beta.-methyl-3-aminomethyl compounds are further changed.

Process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group ONE OF R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen

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Wennigsen, Germany

Akiji Asai