C07C201/12

Gamma amino acid building blocks

The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

FLUID MIXING STRUCTURE, CONTINUOUS REACTION UNIT, CONTINUOUS REACTION REACTOR AND METHOD OF USING THE SAME
20170326520 · 2017-11-16 ·

A fluid mixing structure (10) for mixing at least two fluidic components has a flow inlet port and a flow outlet port and comprises a contraction zone (12), an expansion zone (14), and a retention zone (16), arranged in this order in an inflow direction (IFD) of a fluid flow to flow through said fluid mixing structure (10) and being composed of said at least two fluidic components, and a flow splitter (32) arranged In a space (30) formed by said expansion zone (14) and said retention zone (16) to split said fluid flow in a first sub fluid flow and a second sub fluid flow flowing in a first flow path and a second flow path, respectively, formed in the fluid mixing structure, and to mix said first and second sub fluid flows within said space (30) to generate and discharge a homogenized fluid flow, wherein said flow splitter (32) is arranged and configured to let any flow element of each of said first and second sub fluid flows prior to their mixing have a non-zero average flow component in said inflow direction (IFD).

FLUID MIXING STRUCTURE, CONTINUOUS REACTION UNIT, CONTINUOUS REACTION REACTOR AND METHOD OF USING THE SAME
20170326520 · 2017-11-16 ·

A fluid mixing structure (10) for mixing at least two fluidic components has a flow inlet port and a flow outlet port and comprises a contraction zone (12), an expansion zone (14), and a retention zone (16), arranged in this order in an inflow direction (IFD) of a fluid flow to flow through said fluid mixing structure (10) and being composed of said at least two fluidic components, and a flow splitter (32) arranged In a space (30) formed by said expansion zone (14) and said retention zone (16) to split said fluid flow in a first sub fluid flow and a second sub fluid flow flowing in a first flow path and a second flow path, respectively, formed in the fluid mixing structure, and to mix said first and second sub fluid flows within said space (30) to generate and discharge a homogenized fluid flow, wherein said flow splitter (32) is arranged and configured to let any flow element of each of said first and second sub fluid flows prior to their mixing have a non-zero average flow component in said inflow direction (IFD).

Intermediate for Synthesizing Paroxetine, Method for Preparing the same, and Uses Thereof
20170283380 · 2017-10-05 ·

A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of air organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf).sub.3 to prepare a compound of formula III below: wherein R.sub.1 is alkyl, phenyl or benzyl; R.sub.2, R.sub.3, R.sub.4 are each independently C.sub.1-C.sub.6 alkyl or C.sub.6-C.sub.10 aryl; the chiral amine oxide L has the following structure: wherein n=1, 2; and R=Ph-, 2,6-Me.sub.2C.sub.6H.sub.3-, 2,6-Et.sub.2C.sub.6H.sub.3-, 2,6-iPr.sub.2C.sub.6H.sub.3-, Ph.sub.2CH—.

##STR00001##

CRYSTALLINE FORM OF ELTROMBOPAG FREE ACID

The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation.

##STR00001##

CRYSTALLINE FORM OF ELTROMBOPAG FREE ACID

The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation.

##STR00001##

SOLID-SUPPORTED PALLADIUM (II) COMPLEX AS A HETEROGENEOUS CATALYST FOR CROSS COUPLING REACTIONS AND METHODS THEREOF

A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.

SOLID-SUPPORTED PALLADIUM (II) COMPLEX AS A HETEROGENEOUS CATALYST FOR CROSS COUPLING REACTIONS AND METHODS THEREOF

A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.

SOLID-SUPPORTED PALLADIUM (II) COMPLEX AS A HETEROGENEOUS CATALYST FOR CROSS COUPLING REACTIONS AND METHODS THEREOF

A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.

Metallorganocatalysis for asymmetric transformations

A ligand having the structure or its enantiomer; (I) wherein: each one of R.sub.a, R.sub.b, R.sub.c and R.sub.d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH.sub.2NH; *CH(CH.sub.3)NH(C*,R); and the organocatalyst is an organic molecule catalyst covalently bound to the bridge group. Also, a catalyst having the structure or its enantiomer: (II) wherein: each one of R.sub.a, R.sub.b, R.sub.c and R.sub.d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH.sub.2NH; *CH(CH.sub.3)NH(C*,R); and *CH(CH.sub.3)NH(C*,S); the organocatalyst is an organic molecule catalyst covalently bound to the bridge group; and M is selected from the group consisting of Rh, Pd, Cu, Ru, Ir, Ag, Au, Zn, Ni, Co, and Fe. ##STR00001##