75773-76-1Relevant articles and documents
Tetrahydropyrrole diamine-based bridged bisphenol rare earth metal complex as well as preparation method and application thereof
-
, (2021/09/01)
Ln Is a rare earth metal and a preparation method and an application thereof. R1 And R2 Is selected from tert-butyl, respectively. One of cumyl or triphenyl. The complex provided by the invention has the rare earth element and tetrahydropyrrole diamine base bridging ligand, can effectively catalyze ring opening reaction, and is high in reaction rate, high in activity and mild in reaction condition. The invention further provides a preparation method of the compound shown I. The invention also provides an application of the biodegradable high-molecular material polyhydroxybutyrate (PHB), the ring opening polymerization rate is improved, the preparation method is simpler and easier to control, the yield is high, and the cost is low.
Asymmetric transfer hydrogenation reaction in water: Comparison of chiral proline amide/amine ruthenium(II) complexes
Denizalti, Serpil,Mercan, Deniz,?en, Betül,G?k?e, Ayta? Gürhan,?etinkaya, Bekir
, p. 62 - 66 (2015/02/18)
Chiral proline amide/amine ligands (2, 3), synthesized by multi-step reaction starting from l-proline (1), were evaluated as catalyst generated in situ from [RuCl2(p-cymene)]2 for asymmetric transfer hydrogenation of aromatic ketones in the presence of sodium formiate and sodium dodecyl sulfate (SDS). The results revealed that efficiencies and enantioselectivities strongly depend on the N-substituents.
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic
Hashimoto, Kentaro,Saito, Bunnai,Miyamoto, Naoki,Oguro, Yuya,Tomita, Daisuke,Shiokawa, Zenyu,Asano, Moriteru,Kakei, Hiroyuki,Taya, Naohiro,Kawasaki, Masanori,Sumi, Hiroyuki,Yabuki, Masato,Iwai, Kenichi,Yoshida, Sei,Yoshimatsu, Mie,Aoyama, Kazunobu,Kosugi, Yohei,Kojima, Takashi,Morishita, Nao,Dougan, Douglas R.,Snell, Gyorgy P.,Imamura, Shinichi,Ishikawa, Tomoyasu
, p. 1228 - 1246 (2013/03/28)
To develop novel inhibitor of apoptosis (IAP) proteins antagonists, we designed a bicyclic octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline bioisostere. This design was based on the X-ray co-crystal structure of four N-terminal amino acid residues (AVPI) of the second mitochondria-derived activator of caspase (Smac) with the X-chromosome-linked IAP (XIAP) protein. Lead optimization of this scaffold to improve oral absorption yielded compound 45, which showed potent cellular IAP1 (cIAP1 IC50: 1.3 nM) and XIAP (IC50: 200 nM) inhibitory activity, in addition to potent tumor growth inhibitory activity (GI50: 1.8 nM) in MDA-MB-231 breast cancer cells. X-ray crystallographic analysis of compound 45 bound to XIAP and to cIAP1 was achieved, revealing the various key interactions that contribute to the higher cIAPI affinity of compound 45 over XIAP. Because of its potent IAP inhibitory activities, compound 45 (T-3256336) caused tumor regression in a MDA-MB-231 tumor xenograft model (T/C: -53% at 30 mg/kg).