Patent classifications
C07C303/32
PROCESS FOR PREPARING OSIMERTINIB OR A SALT THEREOF
Provided herein are improved processes and methods for preparing osimertinib or a salt thereof, in particular osimertinib mesylate. The improved process removes the necessity of isolating the unstable aniline intermediate of formula (III) and enables the direct coupling to form the amide product of formula (II):
##STR00001##
The present invention is suitable for a large-scale production, avoiding the isolation of unstable intermediate, thereby providing osimertinib or a mesylate salt thereof in both high yields and high purity.
Unsaturated fatty alcohol derivatives from natural oil metathesis
- David R. Allen ,
- Marcos Alonso ,
- Mary Beddaoui ,
- Randal J. Bernhardt ,
- Aaron Brown ,
- Scott Dillavou ,
- Xue Min Dong ,
- Wilma Gorman ,
- John C. Hutchison ,
- Gary Luebke ,
- Renee Luka ,
- Franz Luxem ,
- Andrew D. Malec ,
- Ronald A. Masters ,
- Dennis S. Murphy ,
- Nicholas Pendleton ,
- Irma Ryklin ,
- Patti Skelton ,
- Brian Sook ,
- Chris SPAULDING ,
- Krista Turpin ,
- Gregory Wallace ,
- Michael Wiester ,
- Patrick Shane Wolfe
Sulfate and sulfonate derivatives of unsaturated fatty alcohols, processes for making them, and methods of using them are disclosed. In one aspect, a monounsaturated fatty alcohol composition is made by reducing a metathesis-derived monounsaturated alkyl ester. The fatty alcohol composition is then converted to a sulfate or sulfonate derivative by one or more of alkoxylation, sulfation, sulfonation, and sulfitation. Of particular interest are the sulfate and ether sulfate derivatives. Microscopy studies indicate that the unsaturated sodium sulfates in particular have a lamellar phase that should enable formulation at high actives levels. Sulfate compositions comprising 40 to 60 wt. % of a monounsaturated fatty primary alcohol sulfate and 40 to 60 wt. % of a secondary hydroxyalkyl primary alcohol sulfate are also disclosed. The derivatives and sulfate compositions are valuable for many end-use applications, including, for example, agricultural dispersants, water-soluble herbicides, anionic emulsifiers for agricultural use, hard surface cleaners, light-duty liquid detergents, personal cleansers, gas well foamers for oilfield applications, laundry detergents, enhanced oil recovery compositions, latex paints, and specialty foams.
Unsaturated fatty alcohol derivatives from natural oil metathesis
- David R. Allen ,
- Marcos Alonso ,
- Mary Beddaoui ,
- Randal J. Bernhardt ,
- Aaron Brown ,
- Scott Dillavou ,
- Xue Min Dong ,
- Wilma Gorman ,
- John C. Hutchison ,
- Gary Luebke ,
- Renee Luka ,
- Franz Luxem ,
- Andrew D. Malec ,
- Ronald A. Masters ,
- Dennis S. Murphy ,
- Nicholas Pendleton ,
- Irma Ryklin ,
- Patti Skelton ,
- Brian Sook ,
- Chris SPAULDING ,
- Krista Turpin ,
- Gregory Wallace ,
- Michael Wiester ,
- Patrick Shane Wolfe
Sulfate and sulfonate derivatives of unsaturated fatty alcohols, processes for making them, and methods of using them are disclosed. In one aspect, a monounsaturated fatty alcohol composition is made by reducing a metathesis-derived monounsaturated alkyl ester. The fatty alcohol composition is then converted to a sulfate or sulfonate derivative by one or more of alkoxylation, sulfation, sulfonation, and sulfitation. Of particular interest are the sulfate and ether sulfate derivatives. Microscopy studies indicate that the unsaturated sodium sulfates in particular have a lamellar phase that should enable formulation at high actives levels. Sulfate compositions comprising 40 to 60 wt. % of a monounsaturated fatty primary alcohol sulfate and 40 to 60 wt. % of a secondary hydroxyalkyl primary alcohol sulfate are also disclosed. The derivatives and sulfate compositions are valuable for many end-use applications, including, for example, agricultural dispersants, water-soluble herbicides, anionic emulsifiers for agricultural use, hard surface cleaners, light-duty liquid detergents, personal cleansers, gas well foamers for oilfield applications, laundry detergents, enhanced oil recovery compositions, latex paints, and specialty foams.
SULFONIUM SALT PHOTOINITIATOR, PREPARATION METHOD THEREFOR, PHOTOCURABLE COMPOSITION COMPRISING SULFONIUM SALT PHOTOINITIATOR, AND USE THEREOF
The present invention provides a sulfonium salt photoinitiator, a preparation method therefor, a photocurable composition comprising sulfonium salt photoinitiator, and use thereof. The sulfonium salt photoinitiator has a structure represented by formula (I). By modifying the structure of an existing sulfonium salt photoinitiator, a sulfonium salt photoinitiator having a new structure is obtained, which can exhibits a higher photosensitivity and an excellent as well as characteristics of low odor and low toxicity, when being used in a photocurable composition. This is significantly superior to existing similar photoinitiators.
##STR00001##
Phenothiazine diaminium salts and their use
- Colin Marshall ,
- Scott Clunas ,
- John Mervyn David Storey ,
- James Peter Sinclair ,
- Thomas Craven Baddeley ,
- Ahtsham Ishaq ,
- Michael Simpson ,
- Craig Williamson ,
- Barry Alan Wood ,
- Claude Michel Wischik ,
- Charles Robert Harrington ,
- Janet Elizabeth Rickard ,
- David Horsley ,
- Yin Sze Loh ,
- Karrar Ahmad Khan ,
- Christopher Paul Larch
Disclosed are compounds of general formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.
Process for preparing safinamide
The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process of the present invention is suitable for the production of safinamide and its salts, preferably safinamide methanesulfonate, at industrial scale.
Process for preparing safinamide
The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process of the present invention is suitable for the production of safinamide and its salts, preferably safinamide methanesulfonate, at industrial scale.
PROCESS FOR PREPARATION OF GLYCOPYRROLATE TOSYLATE
Disclosed herein is an efficacious process for preparation of highly purified Glycopyrrolate tosylate in high yield. The process is being cost effective, environment friendly and easily scalable to high volume industrial production.
PROCESS FOR PREPARATION OF GLYCOPYRROLATE TOSYLATE
Disclosed herein is an efficacious process for preparation of highly purified Glycopyrrolate tosylate in high yield. The process is being cost effective, environment friendly and easily scalable to high volume industrial production.
PROCESS FOR PREPARATION OF GLYCOPYRROLATE TOSYLATE
Disclosed herein is an efficacious process for preparation of highly purified Glycopyrrolate tosylate in high yield. The process is being cost effective, environment friendly and easily scalable to high volume industrial production.