A Novel and Efficient Route for Synthesis of Taladegib

2017 ◽  
Vol 41 (2) ◽  
pp. 112-115 ◽  
Author(s):  
Mingliang Guo ◽  
Kwon Ho Hong ◽  
Yongfeng Lv ◽  
Yu Ding ◽  
Congcong Li ◽  
...  
Keyword(s):  
Large Scale ◽  
Coupling Reaction ◽  
Biological Evaluation ◽  
Reaction Yield ◽  
Scale Production ◽  
Cross Coupling Reaction ◽  
Large Scale Production ◽  
Synthetic Procedure ◽  
Efficient Route ◽  
Hedgehog Signalling Pathway

Taladegib (LY-2940680), a small molecule Hedgehog signalling pathway inhibitor, was obtained from N-benzyl-4-piperidone via Borch reductive amination, acylation with 4-fluoro-2-(trifluoromethyl)benzoyl chloride, debenzylation, substitution with 1,4-dichlorophthalazine and Suzuki cross-coupling reaction with 1-methyl-1H-pyrazole-5-boronic acid. The advantages of this synthesis route were the elimination of Boc protection and deprotection and the inexpensive starting materials. Furthermore, the debenzylation reaction was achieved with simplified operational procedure using ammonium formate as hydrogen source that provided high reaction yield. This synthetic procedure was suitable for large-scale production of the compound for biological evaluation and further study.

The Synthesis of Novel Organic Light-Emitting Material 2,7-Dibromo-2′,3′,6′,7′-Tetra(2-Methylbutyloxy)spirobifluorene

2011 ◽  
Vol 287-290 ◽  
pp. 270-275 ◽  
Author(s):  
Xiao Xia Sun ◽  
Ying Chun Li ◽  
Xi Mei Liu ◽  
Xiao Xiao Zhuang ◽  
Ya Zhou Lou
Keyword(s):  
Large Scale ◽  
Coating Process ◽  
Scale Production ◽  
Light Emitting ◽  
Good Solubility ◽  
Full Color ◽  
Organic Light ◽  
Large Scale Production ◽  
Synthetic Procedure ◽  
Process Ability

A mide, simple and efficient synthetic procedure for the preparation of 2,7-dibromo-2′,3′,6′,7′-tetra(2-methylbutyloxy)spirobifluorene and key intermediates, tetra(2-methlbutyloxy)biphenyl ，2-bromo-4,5,3′,4′-tetra(2-methylbutyloxy)biphenyl, 2,7-Dibromo-2′,6,3′,7′--tetra(2-methylbutyloxy)biphenyl-9-Fluorenol, has been developed. The procedure described herein offers several advantages, including high product yields, easy purification, and large scale production. Ether protected 2,7-dibromo-9,9′-spirobifluorene has good solubility in organic aolvents to permit an appropriate coating process, ability to achieve various colors so as to make full color display elements possible.

scholarly journals Scalable Synthesis of Mesoporous TiO2 for Environmental Photocatalytic Applications

Materials ◽  
2019 ◽  
Vol 12 (11) ◽  
pp. 1853 ◽  
Author(s):  
Francesca Petronella ◽  
Alessandra Truppi ◽  
Massimo Dell’Edera ◽  
Angela Agostiano ◽  
M. Lucia Curri ◽  
...  
Keyword(s):  
Large Scale ◽  
Clean Energy ◽  
Mesoporous Tio2 ◽  
Water Remediation ◽  
Radiation Absorption ◽  
Reaction Yield ◽  
Hydroxyl Groups ◽  
Scale Production ◽  
High Reaction ◽  
Large Scale Production

Increasing environmental concern, related to pollution and clean energy demand, have urged the development of new smart solutions profiting from nanotechnology, including the renowned nanomaterial-assisted photocatalytic degradation of pollutants. In this framework, increasing efforts are devoted to the development of TiO2-based nanomaterials with improved photocatalytic activity. A plethora of synthesis routes to obtain high quality TiO2-based nanomaterials is currently available. Nonetheless, large-scale production and the application of nanosized TiO2 is still hampered by technological issues and the high cost related to the capability to obtain TiO2 nanoparticles with high reaction yield and adequate morphological and structural control. The present review aims at providing a selection of synthetic approaches suitable for large-scale production of mesoporous TiO2-based photocatalysts due to its unique features including high specific surface area, improved ultraviolet (UV) radiation absorption, high density of surface hydroxyl groups, and significant ability for further surface functionalization The overviewed synthetic strategies have been selected and classified according to the following criteria (i) high reaction yield, (ii) reliable synthesis scale-up and (iii) adequate control over morphological, structural and textural features. Potential environmental applications of such nanostructures including water remediation and air purification are also discussed.

scholarly journals Study on optimization of ternary complex of piroxicam-β-cyclodextrin-lysine inclusion in supercritical CO2

2021 ◽  
Vol 63 (3) ◽  
pp. 18-23
Author(s):  
Phan Minh Vuong ◽  
◽  
Do Huu Duy Khoa ◽  
Phan Thanh Thao ◽  
◽  
...  
Keyword(s):  
Large Scale ◽  
Bioactive Compound ◽  
Reaction Yield ◽  
Scale Production ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Large Scale Production ◽  
Maximum Reaction ◽  
Vis Spectroscopy ◽  
Low Solubility

Piroxicam is a bioactive compound classified as a non-steroidal anti-inflammatory drug (NSAID). However, its low solubility in water imposes a serious limitation for its application in the pharmaceutical industry. Using cyclodextrins to form complexes can enhance the dissolution rate, solubility, and bioavailability of piroxicam. In this study, piroxicam/β-cyclodextrin complexes are prepared in supercritical carbon dioxide (SC-CO2) in the solid state and the process was optimized using response surface methodology (RSM). UV-Vis spectroscopy, differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and dissolution profile in water were used to characterized the complex under optimized temperature, residence time, moisture, and ternary agent. Finally, the maximum reaction yield of the inclusion complex was predicted to be 95% at the optimal conditions of 266 bar, 136oC, 1.84:1 ratio of cyclodextrin:piroxicam, and 1.5:1 ratio of lysine:piroxicam. Large scale production of inclusion complexes can be developed from the results of this work on optimizing conditions.

The New Synthesis of Novel Organic Light-Emitting Material Spirobifluorene by Ullman Coupling

2012 ◽  
Vol 204-208 ◽  
pp. 4051-4054
Author(s):  
Ya Zhou Lou ◽  
Xiao Xia Sun ◽  
Ying Chun Li
Keyword(s):  
Large Scale ◽  
Scale Production ◽  
Light Emitting ◽  
Good Solubility ◽  
Full Color ◽  
Organic Light ◽  
Large Scale Production ◽  
New Synthesis ◽  
Synthetic Procedure ◽  
Process Ability

A mide, simple and efficient synthetic procedure for the preparation of 2,7-dibromo-2′,3′,6′,7′-tetra(2-methylbutyloxy)spirobifluorene and key intermediates, tetra(2-methlbutyloxy)biphenyl ，2-bromo-4,5,3′,4′-tetra(2-methylbutyloxy)biphenyl, 2,7-Dibromo-2′,6,3′,7′--tetra(2-methylbutyloxy)biphenyl-9-Fluorenol, has been developed. The procedure described herein offers several advantages, including high product yields, easy purification, and large scale production. Ether protected 2,7-dibromo-9,9′-spirobifluorene has good solubility in organic aolvents to permit an appropriate coating process, ability to achieve various colors so as to make full color display elements possible.

The Synthesis and Biological Evaluation of Indolactam Alkaloids

Synthesis ◽  
2019 ◽  
Vol 51 (23) ◽  
pp. 4443-4451
Author(s):  
Manuel Mendoza ◽  
Ryan Eom ◽  
Celeste Salas ◽  
Jeremy Haynes-Smith ◽  
Kelvin L. Billingsley
Keyword(s):  
Cellular Response ◽  
Large Scale ◽  
Biological Evaluation ◽  
Scale Production ◽  
Synthetic Strategy ◽  
Kinase C ◽  
Large Scale Production ◽  
Lactam Ring ◽  
Synthesis And Biological Evaluation

In this work, we execute a general synthetic strategy to access novel indolactam alkaloids, which are agonists of protein kinase C. This protocol allowed for the most efficient reported syntheses of indolactam V (ILV) stereoisomers, while also affording the large-scale production of natural product (–)-ILV. Structure–activity studies were conducted with these compounds to elucidate the elements necessary to promote PKC-mediated cellular response. EC50 measurements in leukemia and lymphoma cell lines, as well as molecular docking analyses with the PKCδ C1B domain, provided the foundation for these studies. A distinct correlation between in vitro activity and the conformation of the macrocyclic lactam ring was discovered, which can guide design efforts for therapeutics that target the PKC regulatory domain.

The Synthesis of Novel Chiral Organic Light-Emitting Material: 2R,3R-Di(tert-Butanesulfiny)Thiophene

2011 ◽  
Vol 337 ◽  
pp. 151-154 ◽  
Author(s):  
Xiao Xiao Zhuang ◽  
Xiao Xia Sun ◽  
Li Li ◽  
Ying Chun Li
Keyword(s):  
Organic Solvents ◽  
Large Scale ◽  
Scale Production ◽  
Light Emitting ◽  
Product Yields ◽  
Good Solubility ◽  
Organic Light ◽  
Large Scale Production ◽  
Synthetic Procedure

A mide, simple and efficient synthetic procedure for the preparation of 2,3-di(tert-butanesulfiny)Thiophene and key intermediates, chiral tert-Butanethiosulfinate have been developed. The procedure described herein offers several advantages, including high product yields, easy purification, and large scale production. 2,3-di(tert-butanesulfiny)Thiophene has good solubility in organic solvents.

I. S. A. Baud. Forms of Production and Women's Labour: Gender Aspects of Industrialisation in India and Mexico. New Delhi: Sage Publications. 1992. 321 pp.Hardbound. Price: Indian Rs 295.00.

1993 ◽  
Vol 32 (1) ◽  
pp. 129-131
Author(s):  
Naureen Talha
Keyword(s):  
Large Scale ◽  
Indian Society ◽  
New Delhi ◽  
Scale Production ◽  
Female Labour ◽  
Self Employment ◽  
Commodity Production ◽  
Large Scale Production ◽  
Mexican Society ◽  
Small Production

The literature on female labour in Third World countries has become quite extensive. India, being comparatively more advanced industrially, and in view of its size and population, presents a pictures of multiplicity of problems which face the female labour market. However, the author has also included Mexico in this analytical study. It is interesting to see the characteristics of developing industrialisation in two different societies: the Indian society, which is conservative, and the Mexican society, which is progressive. In the first chapter of the book, the author explains that he is not concerned with the process of industrialisation and female labour employed at different levels of work, but that he is interested in forms of production and women's employment in large-scale production, petty commodity production, marginal small production, and self-employment in the informal sector. It is only by analysis of these forms that the picture of females having a lower status is understood in its social and political setting.

An Efficient and Improved Process for the Synthesis of Itopride Hydrochloride and Trimethobenzamide Hydrochloride

2018 ◽  
Vol 15 (4) ◽  
pp. 572-575 ◽  
Author(s):  
Ponnusamy Kannan ◽  
Samuel I.D. Presley ◽  
Pallikondaperumal Shanmugasundaram ◽  
Nagapillai Prakash ◽  
Deivanayagam Easwaramoorthy
Keyword(s):  
Large Scale ◽  
Hydroxylamine Hydrochloride ◽  
Scale Production ◽  
One Pot ◽  
Hydrochloride Salt ◽  
Environmental Friendly ◽  
Large Scale Production ◽  
Non Ulcer Dyspepsia ◽  
Itopride Hydrochloride ◽  
Yield And Purity

Aim and Objective: Itopride is a prokinetic agent used for treating conditions like non-ulcer dyspepsia. Itopride is administered as its hydrochloride salt. Trimethobenzamide is used for treating nausea and vomiting and administered as its hydrochloride salt. The aim is to develop a novel and environmental friendly method for large-scale production of itopride and trimethobenzamide. Materials and Methods: Itopride and trimethobenzamide can be prepared from a common intermediate 4- (dimethylaminoethoxy) benzyl amine. The intermediate is prepared from one pot synthesis using Phyrdroxybenzaldehye and zinc dust and further reaction of the intermediate with substituted methoxy benzoic acid along with boric acid and PEG gives itopride and trimethobenzamide. Results: The intermediate 4-(dimethylaminoethoxy) benzylamine is prepared by treating p-hydroxybenzaldehyde and 2-dimethylaminoethyl chloride. The aldehyde formed is treated with hydroxylamine hydrochloride. The intermediate is confirmed by NMR and the purity is analysed by HPLC. Conclusion: Both itopride and trimethobenzamide were successfully synthesized by this method. The developed method is environmental friendly, economical for large-scale production with good yield and purity.

Sign in / Sign up

Export Citation Format

Share Document