- Tests of a Piperidino Mask for the Protection of Functionalized Carbon Sites in Multistep Syntheses
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Primary alkyl chlorides (R-Cl) are easily isolated in excellent yield after treatment of the appropriate N-alkylpiperidines (R-NC5H10) with α-chloroethyl chloroformate.The method is exemplified by the conversion of a variety of alkylpiperidines, including systems with other sensitive functionalities, to the respective chlorides in yields varying from 90 to 97percent.The potential significance of this process in drug congener preparation and in total synthesis is outlined.Similar fragmentations of N-sec-alkylpiperidines are described.
- Olofson, R. A.,Abbott, Duain E.
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p. 2795 - 2799
(2007/10/02)
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- Bis-basic ketones of fluorene and fluorenone
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The novel bis-basic ketones of fluorene and fluorenone of the present invention have antiviral activity when administered orally and parenterally. These compounds are represented by the following formula: STR1 wherein Z is oxygen or H2 ; each A is a straight or branched alkylene chain having from 1 to about 6 carbon atoms; and each Y is A. the group STR2 wherein R1 and R2 are individually hydrogen, (lower)alkyl having from 1 to about 6 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, alkenyl of from 3 to 6 carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group; or B. the group STR3 WHEREIN N IS A WHOLE INTEGER FROM 4 TO 6, AND R3 is hydrogen, (lower)alkyl of 1 to about 4 carbon atoms, phenyl, or benzyl and can be linked to any one of the carbon atoms of the heterocyclic group; or C. the group STR4 wherein X is oxygen or NR4, and R4 is hydrogen or (lower)alkyl of from 1 to about 4 carbon atoms; or D. the group STR5 WHEREIN P IS A WHOLE INTEGER FROM 2 TO 3, AND M IS A WHOLE INTEGER FROM 1 TO 2; OR A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT OF SAID BASE. These new compounds may be prepared by several different methods which are described.
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