86954-06-5Relevant academic research and scientific papers
Hexafluoroisopropanol-Promoted Haloamidation and Halolactonization of Unactivated Alkenes
Qi, Chenxiao,Force, Guillaume,Gandon, Vincent,Leb?uf, David
supporting information, p. 946 - 953 (2020/12/01)
Pyrrolidine and piperidine derivatives bearing halide functional groups are prevalent building blocks in drug discovery as halides can serve as an anchor for post-modifications. In principle, one of the simplest ways to build these frameworks is the haloa
Structure activity relationship of inhibitors specific for prolyl endopeptidase.
Yoshimoto,Tsuru,Yamamoto,Ikezawa,Furukawa
, p. 37 - 43 (2007/10/02)
Structural requirements of N-blocked L-proline derivatives as specific inhibitors for prolyl endopeptidase were investigated using a series of substrate analogs. Replacement of L-proline by its D-isomer remarkably reduced the inhibition. Introduction of a sulfur atom in proline and/or in the penultimate pyrrolidine rings significantly increased the inhibition, but the introduction of oxygen rather diminished the activity. A peptide linkage (acid-amide bond) between the proline and the pyrrolidine ring was also required to keep the inhibitory activity. A benzyloxycarbonyl group was most effective as an N-blocked component of the inhibitors.
Benzazepine and benzothiazepine derivatives
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, (2008/06/13)
Vasodilating activity is exhibited by compounds having the formula STR1 wherein X can be --S--or --CH2 --; and R2 is STR2 depending upon the definition of X.
Palladium-Catalyzed Carbonylation. A New Synthesis of α-Methylene γ-, δ-, and ε-Lactams and -Lactones Including Bicyclic Lactams of Pyrrolizidine and Indolizidine Skeletons
Mori, Miwako,Washioka, Yumiko,Urayama, Takao,Yoshiura, Kagari,Chiba, Katsumi,Ban, Yoshio
, p. 4058 - 4067 (2007/10/02)
The insertion of carbon monoxide into vinyl halides bearing the secondary amine or alcohol with a catalytic amount of Pd(OAc)2 and PPh3 was realized to give five-, six-, and seven-membered lactams and lactones carrying α-methylene groups in fairly good yields.Bicyclic heterocycles, pyrrolizidine and indolizidine derivatives, were also synthesized from pyrrolidine and piperidine derivatives possessing vinyl halide groups in the side chain at the 2-position of the ring by means of palladium-catalyzed carbonylation.
