Patent classifications
C07D213/24
Complexes
The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2).
##STR00001##
R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.23 and R.sub.24, m, E and X are described in the specification.
The invention also provides a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
ABIRATERONE DERIVATIVE, PREPARATION AND APPLICATION THEREOF
Disclosed in the present invention are an abiraterone derivative and preparation method thereof. The abiraterone derivative provided by the present invention shows relatively few abdominal distension phenomena with respect to abiraterone and has better drug effect and tolerance, and pharmacokinetic experiments show that the plasma concentration of M1 after intragastric administration of equal molar dose is significantly higher than that of abiraterone acetate. The prostate cancer inhibiting effect is obviously better than that of abiraterone, and the side effects on the gastrointestinal tract is smaller than that of abiraterone. A compound provided by the present invention also has the effect of treating acne.
ABIRATERONE DERIVATIVE, PREPARATION AND APPLICATION THEREOF
Disclosed in the present invention are an abiraterone derivative and preparation method thereof. The abiraterone derivative provided by the present invention shows relatively few abdominal distension phenomena with respect to abiraterone and has better drug effect and tolerance, and pharmacokinetic experiments show that the plasma concentration of M1 after intragastric administration of equal molar dose is significantly higher than that of abiraterone acetate. The prostate cancer inhibiting effect is obviously better than that of abiraterone, and the side effects on the gastrointestinal tract is smaller than that of abiraterone. A compound provided by the present invention also has the effect of treating acne.
Ruthenium-catalyzed synthesis of biaryl compounds in water
Using a [RuCl.sub.2(arene)].sub.2 complex and a formate source, a directed ortho CH insertion and aryl-aryl coupling sequence in water provides biaryl compounds useful in the preparation of biologically active molecules and intermediates. Reactions may be conducted in the ambient atmosphere. Ruthenium catalysts prepared from [RuCl.sub.2(arene)].sub.2 and a formate source may be prepared in situ or isolated for later use.
Ruthenium-catalyzed synthesis of biaryl compounds in water
Using a [RuCl.sub.2(arene)].sub.2 complex and a formate source, a directed ortho CH insertion and aryl-aryl coupling sequence in water provides biaryl compounds useful in the preparation of biologically active molecules and intermediates. Reactions may be conducted in the ambient atmosphere. Ruthenium catalysts prepared from [RuCl.sub.2(arene)].sub.2 and a formate source may be prepared in situ or isolated for later use.
GLP-1 receptor modulators
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where represents either or both the R and S form of the compound): ##STR00001##
where A, B, C, Y.sub.1, Y.sub.2, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W.sub.1, n, p and q are as defined herein.
Complexes
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). ##STR00001## Also, a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
Complexes
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). ##STR00001## Also, a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
PROCESS
The invention relates to a process for synthesising organic molecules. The invention provides a process for forming an sp.sup.2-sp.sup.3 carbon-carbon bond between a first compound comprising a substituted or unsubstituted aromatic group and a second compound comprising a substituted or unsubstituted aromatic group in the presence of a catalyst, water, and a first base. The process may find use in the preparation of active pharmaceutical ingredients.
PROCESS
The invention relates to a process for synthesising organic molecules. The invention provides a process for forming an sp.sup.2-sp.sup.3 carbon-carbon bond between a first compound comprising a substituted or unsubstituted aromatic group and a second compound comprising a substituted or unsubstituted aromatic group in the presence of a catalyst, water, and a first base. The process may find use in the preparation of active pharmaceutical ingredients.