The amount of each of the active ingredients, the compound of formula I and optionally the thrombolytic agent or the anticoagulant, in the foregoing compositions is such that effective prevention or limitation of perfusion damage upon administration is obtained, where applicable concomitant with effective thrombolysis or with effective prevention of coagulation. A solution of ethyl 1-tert-butyloxycarbonyl 1,2,4-triazolyl pyrrolo 2,3-c! Antagonists: Atypical antipsychotics e. This amounts to a yield of the monohydrate of N,N-bis- 4- cyanobutyl -piperazine equivalent to Scheme 3. Said preparation generally involves the consecutive N-alkylation or reductive N-alkylation of each piperazine nitrogen atom with the appropriate L-moiety or N-arylalkanamide moiety following art-known procedures. The title compound was prepared in the same manner as that described in Example 51 Step areplacing ammonia with methylamine.
FIG ALKYLATION OF PIPERAZINE N-methyl piperazine can be alkylated in an SN1 reaction its hexahydrate are used as anthelmintics. Direct N1-monosubstitution of piperazine by acyl- sulfonyl- or carbamoyl chlorides.
can be prepared by the reaction of piperazine hexahydrate and ( Boc)2O in to unsymmetrical piperazines synthesis by alkylation of ethyl piperazine The best way is to use BOC piperazine, with one of the nitrogengs blocked, and making the alkylation in the other nitrogen, using a base -potassium carbonate.
The residue was triturated with ethyl acetate and the precipitate collected by filtration to give the title compound as a brown solid 4.
Chemglass Life Sciences. New 4- oxialcoxifenil oxy-piperidines for the treatment of heart and kidney failure. Prepared from Intermediate 2 and phenylacetaldehyde using the general reductive amination procedure; mp.
Agonists: Alcohols e.
N alkylation of piperazine hexahydrate
|The fine needles which formed were collected on a filter and these needles then recrystallized from a mixture consisting of 50 ml.
In addition, the alkylene chain Q may be substituted in any position by a hydroxy group giving rise, for example, to a 2-hydroxypropylene or 2-hydroxymethyl-propylene chain Q. After this time the solvent was removed in vacuo and the residue dissolved in water 10 ml.
Dosage unit form as used in the specification and claims herein refers to physically discrete units suitable as unitary dosages, each unit containing a predetermined quantity of active ingredient calculated to produce the desired therapeutic effect, in association with the required pharmaceutical carrier.
USA Process for the preparation of piperazine derivatives Google Patents
Download Citation: Green Chem.
This paper describes the development of a highly chemoselective methodology for the direct mono‐N‐alkylation of primary aliphatic and. This invention relates to the production of N- alkyl piperazines.
Itis well known in the prior art that the direct alkylation of piperazine to produce the. 26 Gen Aniline & Film Corp Preparation of piperazine and piperazine hydrate.
The solvent was evaporated in vacuo using toluene as an azeotrope.
Prepared from Intermediate 2 and benzaldehyde using the general procedure. There is, however, no disclosure nor any suggestion in EP-A of replacing the alkoxypyridine or alkoxypyrimidine substituent with an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl substituent; nor is there any suggestion therein that the range of substituents specified at the 5-position of the indole moiety might be successfully replaced by an optionally substituted five-membered heteroaromatic ring.
USB1 en. This paper describes adaptation of this chemistry to the BAL-based sequence outlined in Scheme 1permitting the BAL-based solid-phase construction of racemic proline and homologues compounds 3 in Figure 1 with simultaneous incorporation into the basic peptide unit 1.
Video: N alkylation of piperazine hexahydrate Sulfur Monochloride (Disulfur Dichloride)
The hydroxy and mercapto derivatives of formula XIX may be prepared by a variety of methods which will be readily apparent to those skilled in the art. In the foregoing definitions the term halo is generic to fluoro, chloro, bromo and iodo; the term C alkyl defines straight and branched chain saturated hydrocarbon radicals having from 1 to 4 carbon atom, such as, for example, methyl, ethyl, propyl, 1-methylethyl, butyl, 1,1-dimethylethyl and the like; the term Ca-salkanediyl defines straight and branched chain saturated bivalent hydrocarbon radicals having from 3 to 5 carbon atoms, such as, for example, 1,3-propanediyl, 1,4-butanediyl and 1,5-pentanediyl.
N alkylation of piperazine hexahydrate
|Raney cobalt. Examples of optional substituents on the group R 1 include halogen, cyano, trifluoromethyl, triazolyl, tetrazolyl, C alkyl-tetrazolyl, hydroxy, C alkoxy, C alkylthio, C alkoxycarbonyl, C alkylcarbonyl, C -alkylsulphonyl, arylsulphonyl, amino, C alkylamino, di C alkylamino, di C alkylaminomethyl, C alkylcarbonylamino, arylcarbonylamino, C alkoxycarbonylamino, N- C alkyl-N- C alkoxycarbonylamino, C alkylsulphonylamino, arylsulphonylamino, C alkylsulphonylaminomethyl, aminocarbonylamino, C alkylaminocarbonylamino, di C alkylaminocarbonylamino, mono- or diarylaminocarbonylamino, pyrrolidinylcarbonylamino, piperidinylcarbonylamino, aminocarbonyl, C alkylaminocarbonyl, di C alkylaminocarbonyl, aminosulphonyl, C alkylaminosulphonyl, di C alkylaminosulphonyl, aminosulphonylmethyl, C alkylaminosulphonylmethyl and di C alkylaminosulphonylmethyl.
Video: N alkylation of piperazine hexahydrate alkylation (isoparaffin alkylation)
Many variations of R 1R 2and R 3 are permitted on this inherently biomimetic scaffold. In the aforementioned cyclodextrin derivatives, the DS degree of substitution, i.