Patent classifications
C07C317/50
METHOD FOR PREPARING INTERMEDIATE FOR USE IN SYNTHESIS OF FLORFENICOL AND COMPOUNDS PREPARED THEREBY
The present invention provides a method for preparing an intermediate of florfenicol, comprising: reacting p-methylthiobenzaldehyde with isocyanoacetate under catalysis of a chiral catalyst. In the reaction, the chiral product is oxidized to form a methylsulfone-substituted product which is subsequently deformylized to obtain the intermediate. In the method of the present invention, the chiral center of the intermediate is directly generated in the first step of reaction, and the yield of the first step reaches 75%-80%, which is significantly higher than the conventional chiral resolution methods (about 40% yield), and the product has high chiral purity. The method of the present invention does not use anhydrous copper sulfate that pollutes the environment, which reduces the environmental pressure. The compound of p-methylthiobenzaldehyde and the compound of isocyanoacetate are used to react to form a chiral intermediate, which has higher material availability and efficiency than linear synthesis methods.
MASS SPECTROMETRY-CLEAVABLE CROSS-LINKER
Provided herein is synthesis of a novel acidic acid residue targeting sulfoxide-containing MS-cleavable homobifunctional cross-linker. The novel mass spectrometry-cleavable cross-linking agents can be used in mass spectrometry to facilitate structural analysis of intra-protein interactions in proteins and inter-protein interactions in protein complexes. Also disclosed herein are data based on the novel MS-cleavable homobifunctional cross-linker that are complimentary to amine-reactive sulfoxide-containing MS-cleavable reagents.
Sulfamoylating reagents
The present invention provides sulfamoylating reagents of formula R.sup.uN.sup.−—S(O).sub.2X.sup.+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and R.sup.u is an amine protecting group or hydrogen.
Sulfamoylating reagents
The present invention provides sulfamoylating reagents of formula R.sup.uN.sup.−—S(O).sub.2X.sup.+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and R.sup.u is an amine protecting group or hydrogen.
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Ronald J. Heemstra ,
- Ronald Ross, Jr. ,
- Kyle DeKorver ,
- Kaitlyn Gray ,
- Daniel I. Knueppel ,
- Peter Vednor ,
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- John F. Daeuble, SR. ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary Crouse ,
- Fangzheng Li ,
- Jeff Nissen ,
- Monica B. Olson ,
- Michelle Riener ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). ##STR00001##
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Ronald J. Heemstra ,
- Ronald Ross, Jr. ,
- Kyle DeKorver ,
- Kaitlyn Gray ,
- Daniel I. Knueppel ,
- Peter Vednor ,
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- John F. Daeuble, SR. ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary Crouse ,
- Fangzheng Li ,
- Jeff Nissen ,
- Monica B. Olson ,
- Michelle Riener ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). ##STR00001##
Carbocyclic sulfone RORγ modulators
Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##
Carbocyclic sulfone RORγ modulators
Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. ##STR00001##
Compounds Useful for Treating a Mannheimia Haemolytica or Histophilus Somni Infection
The present invention discloses compounds that are useful in the treatment of respiratory diseases of animals, especially Bovine or Swine Respiratory disease (BRD and SRD).
Compounds Useful for Treating a Mannheimia Haemolytica or Histophilus Somni Infection
The present invention discloses compounds that are useful in the treatment of respiratory diseases of animals, especially Bovine or Swine Respiratory disease (BRD and SRD).