Provided herein are methods of using KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Provided herein are methods of using KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Provided herein are KRAS G12C inhibitors, compounds of formula (II), or a pharmaceutically acceptable salt thereof: ##STR00001##
compositions of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Provided herein are KRAS G12C inhibitors, compounds of formula (II), or a pharmaceutically acceptable salt thereof: ##STR00001##
compositions of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

The invention relates to a process for preparing 1,2-benzisothiazoline-3-one according to formula (I), comprising the following steps: (a) reacting a 2-halogenbenzonitrile compound of general formula (II) with a reaction mixture, containing: (i) alkaline sulphide and/or alkaline hydrogen sulphide and (ii) an alkyl halide compound, represented by general formula (III): R.sup.1X (III) for producing an intermediate product of general formula (IV), and (b) reacting the intermediate product of general formula (V) obtained in step (a) with a halogenating agent or an oxidant and subsequent reaction of the 2-(alkylsulfoxy)benzonitrile with an acid to form 1,2-benzisothiazoline-3-one as well as a halide compound of general formula (V) R.sup.1X (V).

The invention relates to a process for preparing 1,2-benzisothiazoline-3-one according to formula (I), comprising the following steps: (a) reacting a 2-halogenbenzonitrile compound of general formula (II) with a reaction mixture, containing: (i) alkaline sulphide and/or alkaline hydrogen sulphide and (ii) an alkyl halide compound, represented by general formula (III): R.sup.1X (III) for producing an intermediate product of general formula (IV), and (b) reacting the intermediate product of general formula (V) obtained in step (a) with a halogenating agent or an oxidant and subsequent reaction of the 2-(alkylsulfoxy)benzonitrile with an acid to form 1,2-benzisothiazoline-3-one as well as a halide compound of general formula (V) R.sup.1X (V).

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by NO bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.