| 摘要 |
<p>The invention relates to novel bisquaternary ammonium derivatives of 2β, 16β-dipiperidino-5α-androstanes having the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="22" wi="66" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<Chemistry id="chema02" num="0002"><Image id="ia02" he="8" wi="25" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>CH(CH<Sub>3</Sub>)<Sub>2</Sub>; R<Sub>2</Sub> = CH<Sub>3</Sub>, C<Sub>2</Sub>H<Sub>5</Sub> or CH<Sub>2</Sub>CH=CH<Sub>2</Sub>; R<Sub>3</Sub> =CH<Sub>3</Sub>, C<Sub>2</Sub>H<Sub>5</Sub> or CH<Sub>2</Sub>CH=CH<Sub>2</Sub>, with the proviso that R<Sub>2</Sub> and R<Sub>3</Sub> are not CH<Sub>3</Sub> simultaneously; R<Sub>4</Sub> = O or H(βOR<Sub>5</Sub>), wherein R<Sub>5</Sub> = H or aliphatic carbacyl (1-6 C); and X = a halogen atom, to processes for their preparation and to pharmaceutical preparations. The invention also relates to novel 16- monoquaternary analogs as intermediates.</p><p>The compounds possess neuromuscular blocking activity.</p> |
