The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

##STR00001##

The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

##STR00001##

The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

##STR00001##

A resist composition comprising a base polymer and a quencher in the form of an amine compound having an iodized aromatic ring bonded to the nitrogen atom via a divalent hydrocarbon group offers a high sensitivity and minimal LWR or improved CDU, independent of whether it is of positive or negative tone.

In the process of the present invention, cariprazine is prepared by converting (trans-4-amino-cyclohexyl)-acetic acid ethyl ester hydrochloride to trans-4-aminocyclohexyl) acetic acid or its hydrochloride by hydrolysis, from the obtained product with addition of dimethylcarbamoyl derivative as a suitable reagent (trans-4-{[(dimethylamino)carbonyl]amino}cyclohexyl) acetic acid is formed, then the obtained compound is linked to 1-{2,3-dichlorophenyl)˜piperazine in the presence of carboxylic acid activating coupling reagent, and so 1,1-dimethyl-3-[trans-4-(2-oxo-2-(4-(2,3-dichlorophenyl)piperazin-1-yl-ethyl)cyclohexyl] urea is formed, which is converted to cariprazine borane adduct of formula (2) in the presence of reducing agent, and finally the product itself is eliminated directly or is obtained from its salt by a known method. The invention also relates to a group of intermediate compounds that are formed and/or used in the process according to the present invention.

In the process of the present invention, cariprazine is prepared by converting (trans-4-amino-cyclohexyl)-acetic acid ethyl ester hydrochloride to trans-4-aminocyclohexyl) acetic acid or its hydrochloride by hydrolysis, from the obtained product with addition of dimethylcarbamoyl derivative as a suitable reagent (trans-4-{[(dimethylamino)carbonyl]amino}cyclohexyl) acetic acid is formed, then the obtained compound is linked to 1-{2,3-dichlorophenyl)˜piperazine in the presence of carboxylic acid activating coupling reagent, and so 1,1-dimethyl-3-[trans-4-(2-oxo-2-(4-(2,3-dichlorophenyl)piperazin-1-yl-ethyl)cyclohexyl] urea is formed, which is converted to cariprazine borane adduct of formula (2) in the presence of reducing agent, and finally the product itself is eliminated directly or is obtained from its salt by a known method. The invention also relates to a group of intermediate compounds that are formed and/or used in the process according to the present invention.

This invention relates to compounds of formula 1, 2 or 3

##STR00001##

a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

The invention provides compounds having the general formula I: ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

The invention provides compounds having the general formula I: ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

The present invention provides a system for evaporating a radioactive fluid, a method for the synthesis of a radiolabelled compound including this system, and a cassette for the synthesis of a radiolabelled compound comprising this system. The present invention provides advantages over known methods for evaporation of a radioactive fluid as it reduces drastically the amount of radioactive gaseous chemicals that are released in the hot cell. It is gentler and more secure compared to the known process and provides access to radiosyntheic processes that may not been acceptable for safety reasons related to release of volatile radioactive gases during evaporation. In addition, the process yields are higher because the radioactive volatiles are labelled intermediate species.