- Piperidine derivatives having renin inhibiting activity
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Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
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- Unsymmetrical polynitrocarbonates and methods of preparation
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Unsymmetrical carbonates of the formula STR1 are prepared by the following reaction sequence STR2 where R and R' can each be --CH2 C(NO2)3, CH2 CF(NO..2)2, --CH2 CF2 (NO2), --CH2 CCl(NO2)2, --CH2 CF3, --CH2 CCl3, --CH2 C(NO2)2 CH3, or --CH2 CF2 CF2 H, provided that R≠R' and wherein R" is a lower alkyl group of from 1 to 6 carbon atoms. Also included are symmetrical 1,3-bis(halo- and nitroalkyl carbonyldioxy)-2,2-dinitropropanes of the formula STR3 which are synthesis by the following reaction sequence STR4 wherein R and R" are as defined above. The carbonates of this invention are useful as energetic additives to propellants and explosive.
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- Protection of functional groups during reaction and their subsequent restoration
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In the process for preparing an organic compound of the formula in which X is an amino group, a hydroxyl group or a carboxyl group, and A' is the remainder of the molecule, from an organic compound of the formula in which A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula in which Z is --NH--, --O-- or a direct C--C bond, and R is a radical of the formula STR1 IN WHICH Y is a direct C--C single bond, the --CH=CH-- group or an arylene group, R1 to R4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or R1 + r2 and R3 + R4 each independently completes a 5- or 6-membered carbocyclic ring, or R1 and R3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporins.
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- Method of preparation of 3-methylenecephams
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Penicillin sulfoxide derived azetidinone sulfinyl chlorides and related sulfinic acid derivatives are cyclized to 3-methylenecephams by reaction with Friedel-Crafts catalysts or metathetic cation forming agents.
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