180302-07-2

Upstream product

• 76-83-5 trityl chloride 
• 121-44-8 triethylamine 
• 6305-38-0 α-amino-γ-butyrolactone hydrobromide 

Relevant academic research and scientific papers

Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders

Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Arylamino fused pyrimidines

Corticotropin releasing factor (CRF) antagonists of formula I or formula II: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.

Aminopolycarboxylic acids and derivatives thereof

There are provided chelating agents particularly useful for the preparation of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula I wherein n and m are 2, 3 or 4; and A, X, R1 and Z are as defined in the specification.

Aminopolycarboxylic acids and derivatives thereof

There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR1 --NZ--(CHR1)n --A--(CHR1)m --NZ--CHR1 --X wherein (each of the groups Z is a group --CHR1 X or the groups Z together are a group --(CHR1)q --A'--(CHR1)r --, where A' is an oxygen or sulphur atom or a group --N--Y; A is a group --N--Y or A--(CHR1)m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR1)q --A'--(CHR1)r --, A may also represent an oxygen or sulphur atom; each Y, which may be the same or different, is a group --(CHR1)p --N(CHR1 X)2 or a group --CHR1 X; each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R1 ; each R1, which may be the same or different, is a hydrogen atom, a hydroxyalkyl group or an optionally hydroxylated alkoxy or alkoxyalkyl group; n, m, p, q and r are each 2, 3 or 4; with the provisos that at least two nitrogens carry a --CHR1 X moiety wherein X is a carboxyl group or a derivative thereof, that each --CHR1 X moiety is other than a methyl group, and that unless A' is oxygen or sulphur or A is N--(CHR1)p --N(CHR1 X)2 at least one R1 is other than hydrogen) and salts thereof.

Synthesis of N-Trityl-L-homoserine

L-Homoserine was tritylated via its silylated product with Me2SiCl2 or Ph2SiCl2 in 65-68percent yield.Also N-Trt-L-methionine upon treatment with MeI and degradation of the resulting sulfonium salt with KOH yielded N-Trt-L-homoserine in 75percent yield.Bo