91154-08-4Relevant academic research and scientific papers
Iridium-Catalyzed Enantioselective Allyl-Allyl Cross-Coupling of Racemic Allylic Alcohols with Allylboronates
Zheng, Yu,Yue, Bei-Bei,Wei, Kun,Yang, Yu-Rong
supporting information, p. 8035 - 8038 (2019/01/14)
Carreira's iridium-(P, olefin) phosphoramidite-based catalytic system that allows asymmetric allyl-allylboronate cross-coupling with high enantioselectivity is reported. This transformation tolerates a large variety of racemic branched allylic alcohols an
Design, Synthesis, and Evaluation of Metabolism-Based Analogues of Haloperidol Incapable of Forming MPP+-like Species
Lyles-Eggleston,Altundas,Xia,Sikazwe,Fan,Yang,Li,Zhang,Zhu,Schmidt,Vanase-Frawley,Shrihkande,Villalobos,Borne,Ablordeppey
, p. 497 - 508 (2007/10/03)
The long-term, irreversible, Parkinsonism-like side effects of haloperidol have been speculated to involve several mechanisms. More recently, it has been speculated that the metabolic transformation to MPP+-like species may contribute to the Parkinsonism-like side effects. Because BCPP+ and its reduced analogue have been shown to possess the potential to destroy dopamine receptors in the nigrostriatum, we have designed new analogues of haloperidol lacking the structural features necessary to form neurotoxic quaternary species but retaining their dopamine-binding capacity. The most potent agent at the D2 receptor, the homopiperidine analogue 11, was found to be equipotent to haloperidol. It was also of interest to identify analogues with DA binding profiles similar to that of clozapine at the dopamine receptor subtypes. Evaluation of the proposed agents shows that the ratio of D2 to D4 (2) binding of clozapine was mimicked by 7 [Ki(D2) = 33, Ki(D3) = 200, Ki(D4) = 11 nM; Ki(D2)/Ki(D4) = 3] and 9 [Ki(D2) = 44, Ki(D3) = 170, Ki(D4) = 24 nM; Ki(D2)/Ki(D4) = 2]. A preliminary in-vivo testing of compound 7 shows that its behavioral profile is similar to that of clozapine. This profile suggests that there is a need for further evaluation of these two synthetic agents and their enantiomers for efficacy and lack of catalepsy in animal models.
A NEW SYNTHESIS OF trans-2-SUBSTITUTED-2-BUTENE-1,4-DIOLS FROM 2-BUTYNE-1,4-DIOL VIA NUCLEOPHILIC ADDITION OF GRIGNARD REAGENTS
Ishino, Yoshio,Wakamoto, Kohji,Hirashima, Tsuneaki
, p. 765 - 768 (2007/10/02)
trans-2-Substituted-2-butene-1,4-diols were readily obtained by reactions of 2-butyne-1,4-diol with Grignard reagents in good yields.
