The invention relates to a process for preparing a diisocyanate of the formula (A)

##STR00001## where R is selected from the group consisting of alkyl, aryl, and combinations thereof, comprising the following process steps in the indicated order; 1) providing an intermediate of the formula (B) with a process using lysine and urea

##STR00002##

and  where R and each R′ are independently selected from the group consisting of alkyl, aryl, and combinations thereof; and 2) thermolytic cleavage of the intermediate of the formula (B), thereby affording the diisocyanate of the formula (A),
and also to the diisocyanate directly prepared therewith.

The invention relates to a process for preparing a diisocyanate of the formula (A)

##STR00001## where R is selected from the group consisting of alkyl, aryl, and combinations thereof, comprising the following process steps in the indicated order; 1) providing an intermediate of the formula (B) with a process using lysine and urea

##STR00002##

and  where R and each R′ are independently selected from the group consisting of alkyl, aryl, and combinations thereof; and 2) thermolytic cleavage of the intermediate of the formula (B), thereby affording the diisocyanate of the formula (A),
and also to the diisocyanate directly prepared therewith.

The compounds of the present invention are represented by the following compounds having Formula I: ##STR00001##
where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic): ##STR00002##
where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

The compounds of the present invention are represented by the following compounds having Formula I: ##STR00001##
where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic): ##STR00002##
where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

A compound of formula (I)

##STR00001##

wherein n is selected from 3 to 8 and R is hydrogen or a C.sub.1-C.sub.8 alkyl radical, a process for the preparation of the compound and uses of the compound.

A compound of formula (I)

##STR00001##

wherein n is selected from 3 to 8 and R is hydrogen or a C.sub.1-C.sub.8 alkyl radical, a process for the preparation of the compound and uses of the 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 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.

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##