40489-73-4Relevant articles and documents
Mitsunobu Reaction Using Basic Amines as Pronucleophiles
Huang, Hai,Kang, Jun Yong
, p. 6604 - 6614 (2017/07/15)
A novel protocol for extending the scope of the Mitsunobu reaction to include amine nucleophiles to form C-N bonds through the utilization of N-heterocyclic phosphine-butane (NHP-butane) has been developed. Both aliphatic alcohols and benzyl alcohols are suitable substrates for C-N bond construction. Various acidic nucleophiles such as benzoic acids, phenols, thiophenol, and secondary sulfonamide also provide the desired products of esters, ethers, thioether, and tertiary sulfonamide with 43-93% yields. Importantly, C-N bond-containing pharmaceuticals, Piribedil and Cinnarizine, have been synthesized in one step from the commercial amines under this Mitsunobu reaction system.
Oxidation-Reduction Condensation of Diazaphosphites for Carbon-Heteroatom Bond Formation Based on Mitsunobu Mechanism
Huang, Hai,Kang, Jun Yong
supporting information, p. 544 - 547 (2017/02/10)
An efficient oxidation-reduction condensation reaction of diazaphosphites with various nonacidic pronucleophiles in the presence of DIAD as a weak oxidant has been developed for carbon-heteroatom bond formation. This mild process affords structurally diverse tertiary amines, secondary amines, esters, ethers, and thioethers in moderate to excellent yields. The selective synthesis of secondary amines from primary amines has been achieved. Importantly, a practical application to the synthesis of antiparkinsonian agent piribedil has been demonstrated.
(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES
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Page/Page column 16, (2010/06/22)
The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.
DIARYL-CYCLYLALKYL DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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, (2009/10/31)
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted N-cyclylalkyl-diphenylpropanamide derivatives as shown in formula (1).
First example of s-BuLi/(-)-sparteine-mediated chiral deprotonation of a piperazine and proof of the sense of induction
McDermott, Benjamin P.,Campbell, Andrew D.,Ertan, Anne
, p. 875 - 879 (2008/12/22)
This paper describes the first known example of a (-)-sparteine-mediated asymmetric deprotonation of a piperazine. Reaction of tert-butyl 4-tert-butylpiperazine-l-carboxylate with s-BuLi in the presence of (-)-sparteine at -78°C and quenching with carbon
Process for making 11-piperazino-diazepines, oxazepines, thiazepines and azepines
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, (2008/06/13)
This invention concerns a novel process for the preparation of 6-piperazinyl derivatives of morphantridine and corresponding ring-substituted and hereto analogues thereof, comprising reacting a compound of the formula: SPC1 Wherein A is benzene or thiophene, and X is --CH2 -- or a hetero atom or group, with a complex comprising titanium, zirconium, hafnium or vanadium and a corresponding piperazinyl derivative. The end products are in general known and useful as neuroleptics.