本发明涉及公式I的取代咪唑[1,5-a][1,2,4]三唑[1,5-d][1,4]苯二氮杂环己烷衍生物,其中R1为氢、卤素、较低烷基、被卤素取代的较低烷基、较低烷氧基、被卤素取代的较低烷氧基、硝基、环烷基、—O(CH2)mO(CH2)mOH或—C≡C—R′;R2为氢或甲基;R3为较低烷基、被卤素取代的较低烷基、较低烯基、被卤素取代的较低烯基、较低炔基、—(CH2)n-环烷基、—(CR′R″)m—CH3、苯基(未取代或被卤素取代)、吡啶基或噻吩基,每种基未取代或被较低烷基取代、—(CH2)n—NH-环烷基、较低烯基-环烷基、较低炔基-(CR′R″)mOH或较低炔基-苯基,其中苯环未取代或被卤素、CF3、较低烷基或较低烷氧基取代;R′为氢或较低烷基;R″为氢、羟基或较低烷基;n为0、1或2;m为1、2或3;o为1或2;及其药学上可接受的酸盐。这类化合物对GABA A α5受体结合位点具有高亲和力和选择性。因此,该发明还涉及增强认知和治疗像阿尔茨海默病这样的认知障碍的方法。
One-Pot Synthesis of α-Branched <i>N</i>-Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics
作者:Chunhui Dai、Julien Genovino、Bruce M. Bechle、Matthew S. Corbett、Chan Woo Huh、Colin R. Rose、Jianmin Sun、Joseph S. Warmus、David C. Blakemore
DOI:10.1021/acs.orglett.7b00082
日期:2017.3.3
A three-component, titanium-mediated synthesis of α-branched N-acylamines from commercial or readily accessible amides, aldehydes, and organometallic reagents is reported. The transformation proceeds under mild reaction conditions and tolerates a variety of functional groups (including nitrile, carbamate, olefin, basic amine, furan, and other sensitive heteroaromatics) to generate a large umbrella
Disclosed herein is the first general chemo- and site-selective alkylation of C-Br bonds in the presence of COTf, C-Cl and other potentially reactive functional groups, using the air-, moisture-, and thermally stable dinuclear PdI catalyst, [Pd(μ-I)PtBu3 ]2 . The bromo-selectivity is independent of the substrate and the relative positioning of the competing reaction sites, and as such fully predictable
This invention relates to dihydro-benzo[b][1,4]diazepin-2-one derivatives of the formula
1
wherein R
1
, R
2
, X and Y are as defined in the specification and R
3
is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I)
wherein A
1
, A
2
,
R
1
, R
2
, R
3
, R
4
, R
5
and R
6
are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
Air-Stable Secondary Phosphine Oxide or Chloride (Pre)Ligands for Cross-Couplings of Unactivated Alkyl Chlorides
作者:Lutz Ackermann、Anant R. Kapdi、Carola Schulzke
DOI:10.1021/ol100658y
日期:2010.5.21
In situ generated and crystallographically well-defined, isolated palladium complexes derived from seven novel air-stable secondary phosphine oxides or chlorides enabled challenging Kumada−Corriu cross-couplings of unactivatedalkylchlorides bearing β-hydrogens and proved applicable to transformations of alkyl-substituted organometallics.