A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The re...

New coumarin-based chiral thiourea sensor 1 was found to be an enantioselective fluorescent chemosensor for N-Boc-protected proline. The chiral sensor shows lower background fluorescence, and higher fluorescence enhancement with 18 nm blue shifts. Job plot analysis result indicates that sensor 1 can form a 1 : 1 stoichiometric complex and it could be used as a fluorescence sensor for the determ...

The title mol-ecule, C(20)H(31)NO(8), has pseudo-C2 symmetry about the C-N bond, with the bis-(tert-butoxy-carbon-yl)amino group twisted from the benzene ring plane by ca 60° and the bulky tert-butoxy-carbonyl (Boc) groups are orientated away from the substituted aniline group. As part of an anti-bacterial drug discovery programme furnishing analogues of platensimycin, we unexpectedly synthesiz...

A simple, efficient, and eco-friendly protocol for the N-Boc protection of the amine moiety in a variety of compounds with di-tert-butyl dicarbonate under water-acetone catalyst-free conditions is described. The corresponding monocarbamate is obtained in excellent yields on short reaction times. No competitive side reactions such as isocyanate urea and O-Boc were observed. This method represent...

The chemoenzymatic synthesis of heparan sulfate tetrasaccharide (1) and hexasaccharide (2) with a fluorous tag attached at the reducing end is reported. The fluorous tert-butyl dicarbonate ((F)Boc) tag did not interfere with enzymatic recognition for both elongation and specific sulfation, and flash purification was performed by standard fluorous solid-phase extraction (FSPE). Based on an (F)Bo...

/V-/j-Alanyldopamine (NBAD) has attracted a great deal of interest because of its significance in catecholamine metabolism in insects with which phenoloxidase is concerned.1' Kramer et al. synthesized NBADby coupling the acid component of /V-/?-alanine with the amine component of dopamine in aqueous solution.2' Their method, however, required several chromatographic steps to purify the syntheti...

Automatic classification of news articles is a relevant problem due to the large amount of news generated every day, so it is crucial that these news are classified to allow for users to access to information of interest quickly and effectively. Traditional classification systems represent documents as bag-of-words (BoW), which are oblivious to two problems of language: synonymy and polysemy. T...

A seven-step synthetic route has been developed to access the labile C-3 unsubstituted 5-phenylthiomorpholinone system for first time. The key step involved nucleophilic ring opening of Boc-phenylmorpholinone give corresponding methyl ester. sulfur introduction was accomplished through a Mitsunobu reaction yield thioacetate, which then hydrolysed provide thiol acid. Cyclization acid achieved us...

VIDEO ABSTRACT The precise connectivity of inputs and outputs is critical for cerebral cortex function; however, the cellular mechanisms that establish these connections are poorly understood. Here, we show that the secreted molecule Sonic Hedgehog (Shh) is involved in synapse formation of a specific cortical circuit. Shh is expressed in layer V corticofugal projection neurons and the Shh recep...

One of the main challenges in Binary Offset Carrier (BOC) tracking is the presence of multiple peaks in the signal autocorrelation function. Thus, several tracking algorithms, including Bump-Jump, Double Estimator, Autocorrelation Side-Peak Cancellation Technique and pre-filtering have been developed to fully exploit the advantages brought by BOC signals and mitigate the problem of secondary pe...