139155-46-7

Upstream product

• 120-72-9 indole 
• 121-90-4 m-nitrobenzoic acid chloride 

Downstream Products

• 139155-47-8 ethyl 4-<3-(3-nitrobenzoyl)-1H-indol-1-yl>butyrate 
• 225942-87-0 ethyl 4-<3-<3-benzoyl>-1H-indol-1-yl>butyrate 
• 139156-03-9 ethyl 4-<3-(3-aminobenzoyl)-1H-indol-1-yl>butyrate 
• 163136-03-6 [14C]-FK-143 
• 139155-48-9 4-[3-(3-nitrobenzoyl)-1H-indol-1-yl]butyric acid 
• 139155-49-0 4-[3-(3-aminobenzoyl)-1H-indol-1-yl]butyric acid 

Relevant academic research and scientific papers

Process for the preparation of indole derivatives or salts thereof

This invention provides a novel process for the preparation of a 3-acylindole or the salt thereof in a high yield.

4-(Benzoylindolizinyl)butyric acids; novel nonsteroidal inhibitors of steroid 5α-reductase. III

A novel series of indolizinebutyric acids with various benzoyl substituents was synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase, and the structure-activity relationships in this series were studied. We previously reported the structure-activity relationships in a series of indolebutyric acids as well as the discovery of the novel nonsteroidal 5α-reductase inhibitor, FK143. We have now made other modifications to this compound to improve in vivo inhibitory activity. By altering the heterocyclic nucleus and changing the benzoyl substituent we have succeeded in identifying the strongly active compound, FK687, (S)-4-[1-[4-[[1-(4-isobutylphenyl)butyl]oxy]benzoyl]indolizin-3-yllbutyric acid, which displays strong in vitro inhibitory activity against the human enzyme and in vivo inhibitory activity against the castrated young rat model. This compound should be a useful agent for the treatment of benign prostatic hyperplasia.

4-(1-benzoylindol-3-yl)butyric acids and FK143: Novel nonsteroidal inhibitors of steroid 5α-reductase (II)

A novel series of indolebutyric acids with varying benzoyl substituents were synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase. We previously reported the discovery of a novel nonsteroidal 5α-reductase inhibitor, FR119680, which had a

INDOLE DERIVATIVES AND THEIR USE FOR TESTOSTERONE 5-ALPHA-REDUCTASE-MEDIATED DISEASES

Indole derivatives of the formula and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia, acnes and prostatism