Case Study 3
Finding new binding sites for human haemoglobin which can alter the oxygen binding capacity of the protein.
Area 1 was to be modified to accommodate cyclic structures instead of a germinal dimethyl and area 2 was to be modified to unsymmetrically substituted 3, 5- dialkyl substituted anilines. Area 1 modification was achieved as follows.
The Protocol followed as below worked with acetone only
It was changed as below
the dialkyl bromides were avaible comercially but some cycloalkyl bromides were prepared as follows
The modifications in the area 2 required to synthesize the 3,5-dialkyl anilines which were carrying different alkyl groups, which was done as follows.
The synthesis was doen as follows
These two goals were achieved in eight months with one FTE. The clinical candidate shown below was also scaled up to one hundred grams for preclinical animal toxicity.
