摘要:
The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide α-substituted-γ-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected γ2-amino acids, which are essential for systematic conformational studies of γ-peptide foldamers.
摘要:
Novel routes for the preparation of acetonylbenzamides are provided by the reaction of an amine and acyl chloride. Novel routes to various intermediates used in the manufacture of acetonylbenzamides are also disclosed.
摘要:
Preparation of N-alkenyl carboxamides of the general formula I ##STR1## in which the radicals R.sup.1 to R.sup.4 independently stand for hydrogen or for aliphatic, cycloaliphatic, or aromatic radicals, which optionally carry inert substituents, wherein an amide of the general formula II ##STR2## in which the radical R.sup.1 has the above meaning, and a carbonyl compound of the general formula III ##STR3## in which the radicals R.sup.2 to R.sup.4 have the above meanings, are caused to react in the presence of a base, said reaction being either a) carried out in the presence of a carboxylic acid derivative of the general formula IV ##STR4## in which the radical R.sup.5 stands for hydrogen or an alkyl or aryl group and X is a halogen, alkoxy, or carboxylalkyl radical, or b) continued in the presence of a carboxylic acid derivative of the formula IV, and the amide of the formula I is isolated.
摘要:
Disclosed is a process for the preparation of aqueous solutions of acetoacetamide wherein diketene and aqueous ammonia having an ammonia concentration of about 6.0 to 9.0 weight percent are continuously fed to a reaction zone at rates which maintain in the reaction zone a pH of about 7.0 to 8.2 and a residence time of about 20 to 150 minutes while (i) maintaining the temperature of the reaction zone at about 40.degree. to 75.degree. C. and (ii) subjecting the contents of the reaction zone to vigorous agitation. An aqueous product solution having an acetoacetamide concentration of about 25 to 35 weight percent is continuously removed from the reaction zone.
摘要:
The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.
摘要:
A process for preparing acetoacetarylamides of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different alkyl radicals,l and m are each 0, 1 or 2, andis 0 or 1,by addition of diketene to the appropriate arylamine by continuously reacting the arylamine with diketene in the presence of a mixture of water and of a (C.sub.1 -C.sub.4)-alkanol at temperatures from 60.degree. C. to 100.degree. C. in the course of from 0.1 to 10 min.
摘要:
A process for the preparation of N-acyl-N-allylaniline. A solution of diallylaniline or a mixture of monoallyl and diallylaniline is placed in contact with a carboxylic acid halide.
摘要:
The new compound 4-chloro-4-chloromethyloxetan-2-one can be prepared by reacting diketene with sulphuryl chloride under conditions in which free radicals are formed.The 4-chloro-4-chloromethyloxetan-2-one exhibits antimicrobial activity. It is also useful as an intermediate, for example for the production of pigments and dyestuffs.
摘要:
The new compound 4-chloro-4-chloromethyloxetan-2-one can be prepared by reacting diketene with sulphuryl chloride under conditions in which free radicals are formed.The 4-chloro-4-chloromethyloxetan-2-one exhibits antimicrobial activity. It is also useful as an intermediate, for example for the production of pigments and dyestuffs.
摘要:
A process for the manufacture of .beta.-isobutyrylaminocrotonic acid amide by reacting .beta.-aminocrotonic acid amide with dimethylketene in the liquid or gaseous state without the application of external heat at temperatures in the range of from room temperature to 70.degree. C. The dispersion medium used is an organic solvent having a boiling point above 40.degree. C. that may contain up to 0.1 mole of water and 0.2 to 2 moles of a carboxylic acid having 1 to 4 carbon atoms per mole of .beta.-aminocrotonic acid amide. If the dimethylketene is added undiluted the reaction is carried out in the absence of oxygen and in the presence of a protective gas atmosphere. The .beta.-isobutyrylaminocrotonic acid amide is obtained in the form of two stereoisomers (Z- and E-forms), which differ as regards their melting point and their solubility in organic solvents. On heating to 40.degree. C., the E-form is converted into the Z-form.