-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

This document discloses molecules having the following formula (Formula One):

##STR00001##

and processes associated therewith.

The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline.

##STR00001## wherein R.sub.1 and R.sub.2 represent independent of each other hydrogen, (un)substituted or substituted amine; R.sub.3 and R.sub.4 represent independent of each other hydrogen or halogen.