摘要:
Compounds of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.
摘要:
The compound Me.sub.2 Val--Val--MeVal--Pro--Pro--NHBzl.multidot.HCl is described. It is prepared from Z--Val--Val--MeVal--Pro--OR.sup.1 where Z and R.sup.1 have the meanings stated in the description. The compound shows antineoplastic activity.
摘要:
Compounds of the formula where R1, R2, R3 and R4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.
摘要:
Alpha,beta-substituted acroleins of the general formula I ##STR1## where A and B are identical or different and are each C.sub.1 -C.sub.4 -alkyl, naphthyl, biphenyl or phenyl which may be monosubstituted or polysubstituted by halogen, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, phenoxy or phenylsulfonyl, are prepared by a process in which a compound of the general formula III ##STR2## where A has the above meanings and R.sup.1 and R.sup.2 are identical or different and are each C.sub.1 -C.sub.4 -alkyl or together possess the carbon atoms required to complete a ring, is reacted with a phosphorus compound of the general formula IV or V ##STR3## where B the meanings stated above, R.sup.1 and R.sup.2 are as defined above and X.sup..crclbar. is a halide ion, in the presence of a base. The alpha,beta-substituted acroleins can be further processed to give hydroxymethyloxiranes.
摘要:
Alpha,beta-substituted acroleins of the general formula I ##STR1## where A and B are identical or different and are each C.sub.1 -C.sub.4 -alkyl, naphthyl, biphenyl or phenyl which may be monosubstituted or polysubstituted by halogen, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, phenoxy or phenylsulfonyl, are prepared by a process in which a compound of the general formula III ##STR2## where A has the above meanings and R.sup.1 and R.sup.2 are identical or different and are each C.sub.1 -C.sub.4 -alkyl or together possess the carbon atoms required to complete a ring, is reacted with a phosphorus compound of the general formula IV or V ##STR3## where B the meanings stated above, R.sup.1 and R.sup.2 are as defined above and X.sup..crclbar. is a halide ion, in the presence of a base. The alpha,beta-substituted acroleins can be further processed to give hydroxymethyloxiranes.
摘要:
Alkyl .gamma.-halotiglates of the general formula I ##STR1## where X is Cl or Br and R.sup.2 is alkyl of 1 to 3 carbon atoms, having a high E isomer content, are prepared by a process in which(a) the corresponding 2-methyl-but-3-enoate of the general formula II ##STR2## is reacted with chlorine or bromine in the absence of a solvent and (b) the resulting 2-methyl-3,4-dihalobutyrate of the general formula III ##STR3## is dehydrohalogenated by reaction with a solution of an alkali metal hydroxide in an alcohol R.sup.2 OH, where R.sup.2 has the stated meaning, or in a mixture of water and an alcohol R.sup.2 OH, and the products are further processed to give O,O-dialkyl-.gamma.-phosphonotiglates of the general formula IV ##STR4## where R.sup.1 is alkyl of 1 to 4 carbon atoms and R.sup.2 is alkyl of 1 to 3 carbon atoms, preferably ethyl, by reaction with a trialkyl phosphite and thermal isomerization. The process gives C.sub.5 building blocks which are extremely interesting for polyene chemistry, the said building blocks being obtained in good yields and essentially in the form of the required E isomers.
摘要:
2-aryl-3,4-diazabicyclo[4.n.0]-alk-2-en-5-ones of the formula ##STR1## where m, n, R, R.sup.1, R.sup.2 and R.sup.3 have the stated meanings, are used for the treatment of cardiac insufficiency.
摘要:
The invention relates to a method for the production of biperiden by reacting an exo/endo mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone with a phenyl magnesium compound to form an isomer mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-piperidino-1-propanol, whereby biperiden is obtained therefrom by conversion of said mixture into corresponding hydrochloride, isolation of said hydrochloride, reconversion to the free base and crystallization of said biperiden.
摘要:
A process for preparing ethyl atropate by reacting ethyl phenylacetate with paraformaldehyde in the presence of a base is described and entails employing as ethyl phenylacetate a product which contains not more than 0.03% of the corresponding methyl phenylacetate, and carrying out the reaction in N-methyl-pyrrolidone or N,N-dimethylformamide.
摘要:
Novel 6-(acylaminaryl)-3(2H)-pyridazinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and B have the meanings given in the description, and their preparation are described.The compounds have thrombocyte aggregation-inhibiting activity.