Patent classifications
C07D207/325
Slow release of organoboronic acids in cross-coupling reactions
A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture:
R.sup.1—B-T (I);
where R.sup.1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp.sup.3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pK.sub.B of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
Slow release of organoboronic acids in cross-coupling reactions
A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture:
R.sup.1—B-T (I);
where R.sup.1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp.sup.3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pK.sub.B of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
Pyrazole derivatives
The present invention relates to pyrazole derivatives of formula (X) ##STR00001## wherein ring A is a pyrazole and substituents R.sup.B1, R.sup.B2, n, R.sup.Q1, R.sup.Q2, R.sup.Q3, and R.sup.Q4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.
Pyrazole derivatives
The present invention relates to pyrazole derivatives of formula (X) ##STR00001## wherein ring A is a pyrazole and substituents R.sup.B1, R.sup.B2, n, R.sup.Q1, R.sup.Q2, R.sup.Q3, and R.sup.Q4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.
Method for preparation of fluoro, chloro and fluorochloro alkylated compounds by homogeneous catalysis
The invention discloses a method for preparations of fluoro, chloro and fluorochloro alkylated compounds by homogeneous Pd catalyzed fluoro, chloro and fluorochloro alkylation with fluoro, chloro and fluorochloroalkyl halides in the presence of di(1-adamantyl)-adamantyl-n-butylphosphine and in the presence of 2,2,6,6-tetramethylpiperdine 1-oxyl.
METABOLISM PROBES FOR THERAPY AND DIAGNOSIS
Novel 2-substituted glutamylanides useful as modulators of ASCT2 inhibitors. Compounds of the present invention can be used to treat patients suffering from diseases caused or influenced by abnormal ASCT2 transporter dysfunction.
METABOLISM PROBES FOR THERAPY AND DIAGNOSIS
Novel 2-substituted glutamylanides useful as modulators of ASCT2 inhibitors. Compounds of the present invention can be used to treat patients suffering from diseases caused or influenced by abnormal ASCT2 transporter dysfunction.
Pyrrole derivatives as PLK1 inhibitors
The invention provides compounds of the formula (3): ##STR00001##
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R.sup.1 is selected from various substituents:
R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.4 is selected from various substituents;
R.sup.5 is selected from various substituents;
Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group;
R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b;
Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker;
R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c;
R.sup.b is selected from hydrogen and various substituents;
and R.sup.7 is selected from R.sup.4. The compounds are useful in the treatment of cancers.
Pyrrole derivatives as PLK1 inhibitors
The invention provides compounds of the formula (3): ##STR00001##
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R.sup.1 is selected from various substituents:
R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.4 is selected from various substituents;
R.sup.5 is selected from various substituents;
Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group;
R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b;
Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker;
R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c;
R.sup.b is selected from hydrogen and various substituents;
and R.sup.7 is selected from R.sup.4. The compounds are useful in the treatment of cancers.
PYRROLE DERIVATIVES AS PLK1 INHIBITORS
The invention provides compounds of the formula (3):
##STR00001## or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R.sup.1 is selected from various substituents: R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group; R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group; R.sup.4 is selected from various substituents; R.sup.5 is selected from various substituents; Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group; R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b; Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker; R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c; R.sup.b is selected from hydrogen and various substituents; and R.sup.b is selected from R.sup.4. The compounds are useful in the treatment of cancers.