- Synthesis method of tirofiban hydrochloride intermediate III (by machine translation)
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The invention belongs to the field, of medicine synthesis, and particularly relates to a synthesis method III of tirofiban hydrochloride intermediate. by, reduction of an intermediate I under the action of a sodium borohydride reducing system to obtain intermediate II, intermediate II under Lewis acid chloride in the presence. SOCl2 Reaction conditions of, process are mild III, and N - process operation is simple, the reaction conditions of the reaction yield, product are improved, the product purity is high, and the reaction yield is increased by, times without being subjected to column purification, to improve the clinical medication safety, of the injection using, the standard crude drug product of the pharmacopoeia standard, and is suitable, for industrial production. (by machine translation)
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- Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design
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Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of β-amyloid peptides (pGlu-Aβ) and thus may participate in the pathogenesis of Alzheimer’s disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, Aβ3E?42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions. This potent Aβ-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.
- Hoang, Van-Hai,Tran, Phuong-Thao,Cui, Minghua,Ngo, Van T. H.,Ann, Jihyae,Park, Jongmi,Lee, Jiyoun,Choi, Kwanghyun,Cho, Hanyang,Kim, Hee,Ha, Hee-Jin,Hong, Hyun-Seok,Choi, Sun,Kim, Young-Ho,Lee, Jeewoo
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supporting information
p. 2573 - 2590
(2017/04/03)
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- Nickel-catalyzed cross-coupling of potassium aryl- and heteroaryltrifluoroborates with unactivated alkyl halides
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A method for the cross-coupling of alkyl electrophiles with various potassium aryl- and heteroaryltrifluoroborates has been developed. Nearly stoichiometric amounts of organoboron species could be employed to cross-couple a large variety of challenging heteroaryl nucleophiles. Several functional groups were tolerated on both the electrophilic and the nucleophilic partners. Chemoselective reactivity of C(sp3) - Br bonds in the presence of C(sp2) - Br bonds was achieved.
- Molander, Gary A.,Argintaru, O. Andreea,Aron, Ioana,Dreher, Spencer D.
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supporting information; experimental part
p. 5783 - 5785
(2011/03/18)
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- Oxabispidine compounds useful in the treatment of cardiac arrhyythmias
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There is provided compounds of formula I, wherein R1, R2, R3, R4, R41to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
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- Synthesis of RGD analogs as potential vectors for targeted drug delivery
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RGD analogs bind to integrin receptors with high affinity and therefore have the potential to be used as vectors for the targeted delivery of pharmaceutical agents to designated sites. Critical to this application is the ability to synthesize RGD analogs
- Jiang, Ji,Wang, Wei,Sane, David C.,Wang, Binghe
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p. 357 - 379
(2007/10/03)
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- Process for preparing fibrinogen receptor antagonists
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The invention is a highly efficient synthesis for making compounds of the formula: STR1 wherein: R1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR6, wherein R6 is H or C1-10 alkyl; m is an integer from two to six; and R4 is aryl, C1-10 alkyl, or C4-10 aralkyl.
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- Substituted tetrahydropyridines as central nervous system agents
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Substituted tetrahydropyridines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
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