由β-二甲基氨基乙烯基酮[RC(O)CH CH-NMe 2,其中R Ph,MeO-4-C 6 H 4,F-4- C 6 H 4,Cl-4-C 6 H 4,Br-4-C 6 H 4,O 2 N-4-C 6 H 4,呋喃-2-基,噻吩-2-基,吡咯-2-报道了仅改变反应条件(添加和不添加吡啶)的烷基,Et和CCl 3 ]和盐酸羟胺。
The invention relates to compounds of formula
wherein the substituents are as described in claim
1
. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
Enantio- and diastereoselective hetero-Diels–Alder reactions between 4-methyl-substituted Rawal’s diene and aldehydes catalyzed by chiral dirhodium(II) carboxamidates: catalytic asymmetric synthesis of (−)-cis-aerangis lactone
The first catalytic asymmetric hetero-Diels–Alder (HDA) reaction between 3-tert-butyldimethylsilyloxy-1-dimethylamino-1,3-pentadiene (4-methyl-substituted Rawal’s diene) and aldehydes is described. With 3 mol % of dirhodium(II) tetrakis[N-benzene-fused-phthaloyl-(S)-piperidinonate], Rh2((S)-BPTPI)4, the cycloaddition reaction proceeded exclusively in an endo fashion and gave, after a novel sequential
Assembly of the Limonoid Architecture by a Divergent Approach: Total Synthesis of (±)-Andirolide N via (±)-8α-Hydroxycarapin
作者:Alexander W. Schuppe、Timothy R. Newhouse
DOI:10.1021/jacs.6b12268
日期:2017.1.18
first total synthesis of the limonoid andirolide N using a 12-step sequence from commercially available materials. The final step of this route demonstrates the chemical feasibility of our biosynthetic proposal that andirolide N arises from 8α-hydroxycarapin. The strategic use of a degraded limonoid as a platform for the synthesis of more structurally complex congeners may be a general approach to obtain
我们使用市售材料的 12 步序列报告了柠檬苦素 andirolide N 的首次全合成。该路线的最后一步证明了我们的生物合成方案的化学可行性,即 andirolide N 来自 8α-hydroxycarapin。战略性地使用降解的柠檬苦素作为合成结构更复杂的同类物的平台,可能是获得具有不同功能特性的柠檬苦素的通用方法。
2-Arylhydrazono-3-oxopropanals in heterocyclic synthesis: Synthesis of arylazopyrazole, arylazoisoxazole and dialkylpyridazine-5,6-dicarboxylate derivatives. New one-step synthesis of arylazopyrimidines
作者:Mariam A. Al-Shiekh、Abdellatif M. Salah El-Din、Ebtisam A. Hafez、Mohamed H. Elnagdi
DOI:10.1002/jhet.5570410501
日期:2004.9
A novel synthesis of arylpyrazole, isoxazole, dialkyl 1,6-dihydropyridazine 5,6-dicarboxylate derivatives and a newone-stepsynthesis of azolopyrimidines under microwave-assisted conditions are reported.