CAS: 53473-36-2; 4-(Trifluoromethyl)Hydrocinnamic Acid

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CAS号2062-26-2 反式-2-三氟甲基肉桂酸 | CAS号16642-92-5 4-三氟甲基肉桂酸 | CAS号3984-22-3 2-乙烯基-1,3-二氧戊环 | CAS号402-43-7 对溴三氟甲苯 | CAS号128796-39-4 4-(三氟甲基)苯硼酸 | CAS号79-10-7 丙烯酸 | CAS号455-19-6 对三氟甲基苯甲醛 | CAS号180635-74-9 3-(4-(三氟甲基)苯基)丙-1-醇 | CAS号68755-37-3 6-(三氟甲基)-1-茚满酮 | CAS号166947-09-7 4-(三氟甲基)苯丙醛 | CAS号769172-66-9 N-[2-(3,4-二甲氧基苯...

4-三氟甲基肉桂酸置于palladium On Activated Charcoal,氢气体系中,化学反应生成 3-(4-三氟甲基苯基)丙酸
参考文献:大规模生产almorexant的3,4-二氢异喹啉催化不对称还原:加氢还是转移加氢
标题:大规模生产almorexant的3,4-二氢异喹啉催化不对称还原:加氢还是转移加氢
摘要:提出了几种方法用于对映体选择性合成alorexant的四氢异喹啉核心(act-078573A),一种双orexin受体拮抗剂.最初的临床供应是通过noyori Ru催化的二氢异喹啉前体的不对称转移氢化(ru-Noyori Ath)获得的.规模扩大时,产率和对映选择性均受到侵蚀.广泛的筛选工作确定了taniaphos是通过专用的催化剂预处理方案进行铱催化的不对称氢化反应的配体,最终生产了超过6吨的四氢异喹啉乙酸盐.主要的成本贡献者是taniaphos.通过将ru-Noyori Ath的二氢异喹啉底物转换为其甲磺酸盐,该ath后来成功地还原为实际应用,输送数百公斤的四氢异喹啉,从而显着降低了催化剂成本贡献.比较了这两种方法的绿色和效率指标.
DOI:10.1021/op400268F

专利信息

专利号:EP-1990333-A1
优先权日:2007-05-11
标题 :Process for the preparation of cinacalcet hydrochloride
权利人:SANDOZ AG
摘要:The present invention relates to a process for the preparation of cinacalcet hydrochloride which is industrially feasible and commercially viable. The synthesis of cinacalcet hydrochloride is carried out by the condensation of 3-trifluromethylphenyl propionic acid with R-(+)-1-(lnaphthyl)ethylamine.

专利号:WO-2015131100-A1
优先权日:2014-02-28
标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
发明人：YU JIN-QUAN
权利人:SCRIPPS RESEARCH INST
摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

专利号:CN-112679336-A
优先权日:2020-12-29
标 题 :A kind of method of heterogeneous palladium metal catalyzed synthesis of phenylpropionic acid compounds

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

专利号:US-9878999-B2
优先权日:2011-03-24
标题 :Proteasome chymotrypsin-like inhibition using PI-1833 analogs
发明人：LAWRENCE HARSHANI R; SEBTI SAID M; OZCAN SEVIL
权利人:H LEE MOFFITT CANCER CT & RES
摘要:Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).

专利号:WO-2010011325-A2
优先权日:2008-07-23
标题:Synthesis and utilization of small molecules for the treatment of inflammation associated with interleukin-1 signaling