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JournalISSN: 0936-5214


About: Synlett is an academic journal. The journal publishes majorly in the area(s): Enantioselective synthesis & Catalysis. It has an ISSN identifier of 0936-5214. Over the lifetime, 15984 publication(s) have been published receiving 215539 citation(s).
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Journal ArticleDOI
01 Dec 2021-Synlett
Abstract: We have developed a nickel-catalyzed insertion reaction of an alkyne into a 2-(trifluoromethyl)-1,3-benzothiazole to give a seven-membered benzothiazepine that is converted into a 2-(trifluoromethyl)quinoline by thermal desulfidation. This process can be considered a formal substitution of a sulfur atom with an alkyne. The structure of the thianickelacycle intermediate formed through oxidative addition of a C–S bond in the benzothiazole to nickel(0) was confirmed by X-ray single-crystal structure analysis and in situ X-ray absorption fine-structure spectroscopy.

Journal ArticleDOI
26 Nov 2021-Synlett
Abstract: An eco-friendly protocol to synthesize nitriles from their corresponding aromatic and aliphatic aldehydes in excellent yields has been developed. This is a catalyst-free protocol which employs an aminating reagent (MsONH3OTf) under mild conditions. The hydroxylamine triflic acid salts (MsONH3OTf) acted as the N source for this protocol. Our protocol proved to be easy to perform and presented good functional group tolerance.

Journal ArticleDOI
22 Nov 2021-Synlett
Abstract: In this paper, ynolate-initiated cycloaddition (annulation) to form a range of carbocycles and heterocycles is described. Ynolates consist of a ketene anion equivalent, which contains both nucleophilic and electrophilic moieties, and a carbodianion equivalent that achieves double addition. Hence, in addition to the usual [n+2] cycloaddition, ynolates can perform formal [n+1]-type annulations. Their high-energy performance has been demonstrated by their triple addition to arynes to generate triptycenes, in which the C–C triple bond of ynolates is cleaved. The synthetic applications of these methods, including natural products synthesis, are also described. 1 Introduction 2 Preparation of Ynolates 2.1 Double Lithiation 2.2 Flow Synthesis 2.3 Double Deprotonation 3 [2+2] Cycloaddition to C=O Bond 3.1 To Aldehydes and Ketones 3.2 Sequential Cycloaddition 4 [2+2] Cycloaddition to Imino Groups

Journal ArticleDOI
Hai Van Le1, Loc Van Tran1, Anh Tuan Tran2, Thao Thi Phuong Tran1  +2 moreInstitutions (2)
19 Nov 2021-Synlett
Abstract: Synthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.

Journal ArticleDOI
17 Nov 2021-Synlett
Abstract: The rearrangement of allylic imidates is a powerful transformation for the synthesis of allylic amines. Whereas the [3,3]-rearrangement has long been established as the Overman rearrangement, the corresponding [1,3]-rearrangement is rare. Here, we report a novel strategy for the [1,3]-rearrangement of imidates based on the oxidative addition of a palladium(0) catalyst to an allylic imidate. Structurally distinct allylic amides could be synthesized under mild and base-free conditions.

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