An Efficient, Mild, Solvent-Free, One-Pot Three-Component Mannich Reaction Catalyzed by (C4H12N2)2[BiCl6]Cl·H2O

Lu, Hongfei; Wu, Runze; Cheng, Helong; Nie, Shipeng; Tang, Yan; Gao, Yuhua; Luo, Zhibin

doi:10.1055/s-0034-1380278

Cited by 19 publications

(6 citation statements)

References 4 publications

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“…Such benefits as diversity-oriented synthesis, combinatorial library generation, and convergence/divergence acknowledge many aspects of GC and the sustainable synthesis process. For the purpose of green synthesis, well-known classical MCRs are Biginelli, − Strecker, − Mannich, − Passerini, − Ugi, − Orru, Hantzsch, − Petasis, − Groebke–Blackburn–Bienayme, , Kabachnik–Fields, − Willgerodt–Kindler, Bucherer–Bergs, − Gewald reactions, − etc. The mentioned MCRs are used directly to synthesize many pharmaceuticals and key intermediates following the major principles of GC.…”

Section: Multicomponent Reactions For Green and Sustainable Synthesismentioning

confidence: 99%

“…Lu et al implemented a one-pot Mannich reaction of aldehydes with aromatic ketones and amines under solvent-free conditions at room temperature. The MCR is catalyzed by (C 4 H 12 N 2 ) 2 [BiCl 6 ]Cl·H 2 O, and it can be recycled and reused several times by straightforward isolation procedures without losing the catalytic efficiency.…”

Section: Multicomponent Reactions For Green and Sustainable Synthesismentioning

confidence: 99%

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Green Chemistry in the Synthesis of Pharmaceuticals

et al. 2021

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The principles of green chemistry (GC) can be comprehensively implemented in green synthesis of pharmaceuticals by choosing no solvents or green solvents (preferably water), alternative reaction media, and consideration of one-pot synthesis, multicomponent reactions (MCRs), continuous processing, and process intensification approaches for atom economy and final waste reduction. The GC's execution in green synthesis can be performed using a holistic design of the active pharmaceutical ingredient's (API) life cycle, minimizing hazards and pollution, and capitalizing the resource efficiency in the synthesis technique. Thus, the presented review accounts for the comprehensive exploration of GC's principles and metrics, an appropriate implication of those ideas in each step of the reaction schemes, from raw material to an intermediate to the final product's synthesis, and the final execution of the synthesis into scalable industry-based production. For real-life examples, we have discussed the synthesis of a series of established generic pharmaceuticals, starting with the raw materials, and the intermediates of the corresponding pharmaceuticals. Researchers and industries have thoughtfully instigated a green synthesis process to control the atom economy and waste reduction to protect the environment. We have extensively discussed significant reactions relevant for green synthesis, one-pot cascade synthesis, MCRs, continuous processing, and process intensification, which may contribute to the future of green and sustainable synthesis of APIs. CONTENTS1. Introduction 3638 2. Green Chemistry (GC) 3639 2.1. Definition 3639 2.2. The Principles of GC 3641 2.3. The Metrics of GC 3641 2.3.1. Standardization of the E Factor Concept 3641 2.3.2. Baran's Process Ideality Metric 3641 2.3.3. Identification of Process Complexity 3641 2.3.4. The Green Aspiration Level Concept 3642 2.3.5. Innovation Green Aspiration Level (iGAL) 3642 3. The Choice of Solvents in the Green Synthesis of APIs 3642 4. The Reaction with Green Solvents 3643 4.1. The No-Solvent Process 3644 4.

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Section: Multicomponent Reactions For Green and Sustainable Synthesismentioning

confidence: 99%

Section: Multicomponent Reactions For Green and Sustainable Synthesismentioning

confidence: 99%

Green Chemistry in the Synthesis of Pharmaceuticals

et al. 2021

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“…The iminium derivative of the aldehyde is the acceptor in the reaction. 96 Lu and colleagues 97 implemented a greener Mannich reaction under solvent-free conditions at room temperature (Fig. 12).…”

Section: Towards Greener Reactionsmentioning

confidence: 99%

“…Lu and colleagues 97 implemented a greener Mannich reaction under solvent-free conditions at room temperature (Fig. 12).…”

Section: Less Hazardous Chemical Synthesesmentioning

confidence: 99%