摘要:
Renin-inhibiting peptides of the formula ##STR1## in which X represents a group of the formula ##STR2## represents hydroxyl, alkoxy having up to 8 carbon atoms, benzyloxy or a group of the formula --NR.sup.4 R.sup.5,A, B, D and E are identical or different and in each caserepresent a direct bond,represent a radical of the formula ##STR3## in which Q1 denotes oxygen, sulphur or the methylene grouprepresent a grouping of the formula ##STR4## m represents a number 0, 1 or 2, and L represents a group of the formula --CH.sub.2 NR.sup.2 R.sup.3and physiologically acceptable salts thereof.
摘要:
The process for the reaction of bicyclic amide acetals with reactive protic compounds of the general Formula ##STR1## wherein Y represents a member selected from the group consisting of ##STR2## R.sup.1 represents a member selected from the group consisting of hydrogen, an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, and R.sup.2 represents a member selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, an alkylene ether group having from 1 to 50 carbon atoms, an arylene ether group having from 6 to 50 carbon atoms such as ethyl carbamate to form novel products which are useful as curing agents, blowing agents and monomers is disclosed.
摘要:
A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structure represents (D) of (L) isomers) which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.1 is alkyl, that is ##STR6## such alcohol may be hydrogenated to form the aminoalcohol intermediate. All of the above 7-oxabicycloheptane compounds are novel and also form part of the present invention.
摘要:
1-Benzyl(or substituted benzyl)-3.beta.-[4(S)-aryloxazolidin-2-one-3-yl]-4.beta.-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic .beta.-lactam antibiotics.
摘要:
The invention is a process for the preparation of a N- or S-1,2-ethylenically unsaturated organic compound which comprises(a) contacting a N- or S-silylated organic compound with an aldehyde, wherein the aldehyde has a hydrogen atom bonded to the carbon adjacent to the carbonyl moiety, at elevated temperatures under conditions such that a N- or S-1-siloxyalkyl-substituted organic compound is prepared; and(b) pyrolyzing the N- or S-1-siloxyalkyl-substituted organic compound under conditions such that the siloxy moiety is elminated to prepare a N- or S-1,2-ethylenically unsaturated compound.
摘要:
1,3-Oxazolidine-one derivatives of the following formula ##STR1## where R is straight or branched alkyl of C.sub.3 -C.sub.8, X is hydrogen, halogen, lower alkyl or lower alkoxy and n is 4, 5 or 6, or their acid addition salts are effective for medicinal and agricultural use.
摘要:
The invention is a process for the preparation of 2-oxazolidinones which comprises contacting a 2-hydroxyalkyl carbamate with an alkylene oxide or alkylene carbonate in the presence of a catalytic amount of a quaternary ammonium halide, quaternary phosphonium halide, a group I metal carbonate, hydroxide, oxide or halide, or a group II metal carbonate, hydroxide, oxide or halide under conditions such that a 2-oxazolidinone is prepared.
摘要:
N-alkoxycarbonyl-substituted cyclic lactams and nitrogen-containing cyclic ketones are prepared by reaction of a C.sub.1-20 alkyl ester of trichloroacetic acid with the corresponding cyclic lactam or nitrogen-containing cyclic ketone.