Provided herein are methods and intermediates for making (1R,2R,5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.

Provided herein are methods and intermediates for making (1R,2R,5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.

Provided herein are methods and intermediates for making (1R,2R,5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from ##STR00001##
each of R.sub.1 and R.sub.2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH.sub.2).sub.n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH.sub.2).sub.m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(═O)NH—, —NHC(═O)—; R.sub.3 is selected from substituted or unsubstituted C.sub.1-C.sub.30 alkyl, substituted or unsubstituted C.sub.2-C.sub.30 alkenyl, substituted or unsubstituted C.sub.2-C.sub.30 alkynyl, substituted or unsubstituted C.sub.3-C.sub.30 cycloalkyl, cholane aliphatic group, —R.sup.3a—C(═O)O—R.sup.3b, —R.sup.3a—OC(═O)—R.sup.3b, —R.sup.3a—C(═O)NH—R.sup.3b, —R.sup.3a—NHC(═O)—R.sup.3b, —R.sup.3a—S(═O).sub.1-2O—R.sup.3b and —R.sup.3a—OS(═O).sub.1-2—R.sup.3b. ##STR00002##

The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess.

##STR00001##

The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess.

##STR00001##

Methods of making β-homoamino acids as intermediate for synthesis of peptide monmer and dimer α4β7-antagonists are disclosed. The disclosed methods include solid phase and solution phase methods.