scholarly journals An Efficient Synthesis of 4-Aminomethyl-1-(2-Phenylethyl)-Piperidin-4-ol: A Key Intermediate in Fenspiride HCl Synthesis

2021 ◽  
pp. 139-146
Author(s):  
Prasad Panchabhai ◽  
Neelakandan Kaliaperumal ◽  
Gopalakrishnan Mannathusamy ◽  
Anbuselvan Chinnadurai
Keyword(s):  
Green Chemistry ◽  
Hazardous Waste ◽  
Building Block ◽  
Manufacturing Process ◽  
Good Yield ◽  
Aqueous Ammonia ◽  
Scale Production ◽  
Efficient Synthesis ◽  
Environment Friendly ◽  
Bulk Scale

The article confers a scalable manufacturing process of Fenspiride HCl. 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol is the main building block in Fenspiride HCl synthesis. The reported reagents for 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis are costly, explosive, highly toxic, produce hazardous waste, and also need to be handled with most care. The paper introduces aqueous ammonia as an alternate reagent in Fenspiride HCl and used in 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis. The new green chemistry aspect makes the process environment-friendly and cheaper. It also eliminates toxic, sensitive, and hazardous reagents and makes the process safe on uncomplicated on bulk scale production. The high pure Fenspiride HCl is obtained by following this process and meets the ICH limits with good yield.

scholarly journals Development of an Efficient Route to 2-Ethynylglycerol for the Synthesis of Islatravir

2021 ◽  
Author(s):  
Stephan M. Rummelt ◽  
Ji Qi ◽  
Yonggang Chen ◽  
James F. Dropinski ◽  
Gregory Hughes ◽  
...  
Keyword(s):  
Physical Properties ◽  
Building Block ◽  
Manufacturing Process ◽  
Process Development ◽  
Nucleoside Analog ◽  
Efficient Synthesis ◽  
Efficient Route ◽  
Acid Catalyzed ◽  
Initial Route ◽  
Nucleophile Addition

The unnatural, alkyne-containing nucleoside analog islatravir (MK-8591) is synthetically accessed through a biocatalytic cascade starting from 2-ethynylglycerol as a building block. Herein, we describe the development of an efficient synthesis of this building block including the initial route, route scouting and final process development. Key challenges that have been overcome are the development of an efficient and safe acetylenic nucleophile addition to an appropriate ketone, and the identification of a 2-ethynylpropane-1,2,3-triol derivative with favorable physical properties. An acid-catalyzed cracking of commercially available 1,3-dihydroxyacetone dimer and subsequent 1,2-addition of an acetylenic nucleophile has been discovered and optimized into the manufacturing process

scholarly journals Development of an Efficient Route to 2-Ethynylglycerol for the Synthesis of Islatravir

2021 ◽  
Author(s):  
Stephan M. Rummelt ◽  
Ji Qi ◽  
Yonggang Chen ◽  
James F. Dropinski ◽  
Gregory Hughes ◽  
...  
Keyword(s):  
Physical Properties ◽  
Building Block ◽  
Manufacturing Process ◽  
Process Development ◽  
Nucleoside Analog ◽  
Efficient Synthesis ◽  
Efficient Route ◽  
Acid Catalyzed ◽  
Initial Route ◽  
Nucleophile Addition

The unnatural, alkyne-containing nucleoside analog islatravir (MK-8591) is synthetically accessed through a biocatalytic cascade starting from 2-ethynylglycerol as a building block. Herein, we describe the development of an efficient synthesis of this building block including the initial route, route scouting and final process development. Key challenges that have been overcome are the development of an efficient and safe acetylenic nucleophile addition to an appropriate ketone, and the identification of a 2-ethynylpropane-1,2,3-triol derivative with favorable physical properties. An acid-catalyzed cracking of commercially available 1,3-dihydroxyacetone dimer and subsequent 1,2-addition of an acetylenic nucleophile has been discovered and optimized into the manufacturing process

Efficient Synthesis of DiAZT Triphosphate

2014 ◽  
Vol 662 ◽  
pp. 59-62
Author(s):  
Shan Shan Gong ◽  
Qi Sun
Keyword(s):  
Efficient Method ◽  
Good Yield ◽  
Efficient Synthesis

A facile and efficient method for the synthesis ofP1,P3-dizidovudine-5′,5′-triphosphate has been developed. The coupling of zidovudine diphosphate with zidovudine phosphoropiperidate based on the DCI activation of P-N bond afforded the desired product in good yield.

An efficient synthesis of novel spiro[[8H]indeno[2,1-b]-thiophene-8,9′-fluorene] building block for blue light-emitting materials

2006 ◽  
Vol 47 (36) ◽  
pp. 6421-6424 ◽  
Author(s):  
Ling-Hai Xie ◽  
Ting Fu ◽  
Xiao-Ya Hou ◽  
Chao Tang ◽  
Yu-Ran Hua ◽  
...  
Keyword(s):  
Blue Light ◽  
Building Block ◽  
Efficient Synthesis ◽  
Light Emitting

Eine effiziente Synthesemethode für DiarylallenyIiden(pentacarbonyl)chrom- und -wolfram-Komplexe -Kristallstruktur von (CO)5Cr=C=C=CPh2 / An efficient Synthesis of Diarylallenylidene Pentacarbonyl Chromium and Tungsten Complexes - Crystal Structure of (CO)5Cr=C=C=CPh2

1994 ◽  
Vol 49 (9) ◽  
pp. 1207-1214 ◽  
Author(s):  
Helmut Fischer ◽  
David Reindl ◽  
Gerhard Roth
Keyword(s):  
Crystal Structure ◽  
Structure Analysis ◽  
Good Yield ◽  
Efficient Synthesis ◽  
X Ray ◽  
Tungsten Complexes ◽  
And Tungsten

An efficient synthesis of diarylallenylidene pentacarbonyl chromium and tungsten com­plexes is presented. Irradiation of M(CO)6 in THF affords (CO)sM[THF], Substitution of the THF ligand by diarylpropargylalcoholate and subsequent desoxygenation with COCF gives the title compounds in good yield. (The structure of diphenylallenylidene pentacarbonyl chromium has been determined by X-ray structure analysis

Hydrothermal synthesis, hierarchical structures and properties of blue pigments SrCuSi4O10 and BaCuSi4O10

CrystEngComm ◽  
2014 ◽  
Vol 16 (24) ◽  
pp. 5418-5423 ◽  
Author(s):  
Yan Chen ◽  
Mingyu Shang ◽  
Xiaofeng Wu ◽  
Shouhua Feng
Keyword(s):  
Hydrothermal Synthesis ◽  
Green Chemistry ◽  
High Purity ◽  
Good Yield ◽  
Near Infrared ◽  
Hierarchical Structures ◽  
Infrared Luminescence ◽  
Structures And Properties

In this work, a green chemistry strategy was developed to synthesize blue pigments SrCuSi4O10 and BaCuSi4O10 with good yield and high purity. SrCuSi4O10 and BaCuSi4O10 exhibit hierarchical structures. Our study shows that hydrothermally synthesized BaCuSi2O6 exhibits interesting broad near-infrared luminescence.

Efficient synthesis of 2,3-dimethoxy-5-methyl-6-morpholinomethyl-1,4-benzoquinone hydrochloride

2015 ◽  
Vol 70 (4) ◽  
pp. 221-223 ◽  
Author(s):  
Jin Wang ◽  
Teng-huo-sheng Liao ◽  
Jian Yang
Keyword(s):  
Title Compound ◽  
Good Yield ◽  
Efficient Synthesis ◽  
Reaction Sequence

AbstractThe title compound (5) was prepared by a reaction sequence starting from 2,3,4,5-tetramethoxytoluene (1) via the Blanc reaction, oxidation and alkylation. The described method provides a good yield of the C-6 heterocyclic-substituted benzoquinone derivative and is suitable for the synthesis of other benzoquinone derivatives.

An Improved And Suitable Method For Large Scale Produdcion Of Α-Monochlorocyclodecanone

2021 ◽  
Vol 18 ◽  
Author(s):  
Wenhua Ou ◽  
Ruolin Wang ◽  
Ruonan Liu ◽  
Hong Huang
Keyword(s):  
Silica Gel ◽  
Large Scale ◽  
Raw Materials ◽  
Separation Method ◽  
Suitable Method ◽  
Scale Production ◽  
Reaction Conditions ◽  
Environment Friendly ◽  
Large Scale Production ◽  
Ideal Approach

: α-Monochlorocyclododecanone was synthesized from cyclododecane and 1,3-Dichloro-5,5-dimethylhydantoin (DCDMH) catalyzed with silica gel in MeOH. The product was obtained by crystallization with nearly 85% yield. The presented method used cheap raw materials, mild reaction conditions, simple separation method and environment-friendly process. Additionally, the current synthesis provided an ideal approach for large-scale production.

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