128372-97-4

Upstream product

• 6404-29-1 6-(tert-butoxycarbonylamino)hexanoic acid 
• 74-88-4 methyl iodide 

Downstream Products

• 27219-07-4 5-(N-tert-butyloxycarbonyl)aminopentanoic acid 
• 80860-42-0 tert-butyl 6-oxohexylcarbamate 
• 178172-34-4 tert-butyl 2-hydroxyazepane-1-carboxylate 
• 1309251-02-2 (3S,4S)-4-((3S,4S)-4-((3S,4S)-4-(ε-(N-isovalerylamino)hexanoyl)amino-3-hydroxy-6-methylheptanoylamino)-5-cyclohexyl-3-hydroxypentanoylamino)-3-hydroxy-6-methylheptanoic acid N-isoamylamide 
• 1309434-05-6 (3S,4S)-4-((3S,4S)-4-((3S,4S)-4-(ε-(N-isovalerylamino)hexanoyl)amino-3-hydroxy-6-methylheptanoylamino)-5-cyclohexyl-3-hydroxypentanoylamino)-3-hydroxy-6-methylheptanoic acid ethyl ester 
• 138199-80-1 Z-PrTyr-D-Met-Gly-Phe-εAhx-εAhx-OMe 
• 138199-81-2 Z-iPrTyr-D-Met-Gly-Phe-εAhx-εAhx-OMe 
• 138199-84-5 Z-PrTyr-D-Met-Gly-Phe-εAhx-OMe 
• 138199-85-6 Z-iPrTyr-D-Met-Gly-Phe-εAhx-OMe 
• 138199-83-4 H-iPrTyr-D-Met-Gly-Phe-εAhx-εAhx-OH 
• 138199-82-3 H-PrTyr-D-Met-Gly-Phe-εAhx-εAhx-OH 
• 138199-87-8 H-iPrTyr-D-Met-Gly-Phe-εAhx-OH 
• 138199-86-7 H-PrTyr-D-Met-Gly-Phe-εAhx-OH 
• 138199-75-4 Boc-Gly-Phe-εAhx-εAhx-OMe 

Relevant academic research and scientific papers

New renin inhibitors containing aliphatic or aromatic amides at the C-terminus

Five renin inhibitors, Iva-Pro-Phe(4-OMe)-MeLeu-Sta-εAhx-IAA (18), Iva-εAhx-Phe(4-OMe)-MeLeu-Sta-εAhx-IAA (23), H-εAhx-Phe(4-OMe)-His-Sta-εAhx-FBZA (36), H-εAhx-Phe(4-OMe)-His-Sta-εAhx-MBZA (45), and H-Phe (4-OMe)-His-Sta-εAhx-FBZA (48) have been synthesized in search of structures of improved biological properties. All synthesized inhibitors were resistant to chymotrypsin activity. Inhibitors 18 and 23 were insoluble in buffers, pH 7.4 and 2.0, 36, 45 and 48 were very good soluble in buffer pH 2.0 and poorly in buffer pH 7.4. Experimentally determined 1-octanol/pH 7.4 buffer partition coefficients (log P) of 36, 45 and 48 were above 1. Log P values of 18, 23, 36, 45 and 48 were 6.57, 6.91, 2.48, 2.09 and 2.00 respectively. The inhibitory potency in vitro of 18, 23, 36, 45 and 48 expressed as IC50 was 7.5 · 10-5, 5.0 · 10-6, 7.5 · 10-3, 1.0 · 10-4 and 2.5 · 10-5 M/l respectively.

Asymmetric catalysis of intramolecular N-H insertion reactions of α-diazocarbonyls

Intramolecular N-H insertion reactions of α-diazocarbonyl substrates are catalysed by rhodium(II) carboxylates with catalyst-dependent competition with C-H insertion and β-elimination; asymmetric N-H insertion leading to a pipecolic acid derivative with ee up to 45% is achieved using chiral catalysts.

SYNTHESIS OF ENKEPHALIN ANALOGS. PART IV. N-ALKYLATED DERIVATIVES

Four new derivatives of enkephalin analogs: H-PrTyr-D-Met-Gly-Phe-εAhx-εAhx-OH (24).H-iPrTyr-D-Met-Gly-Phe-εAhx-εAhx-Oh (25).H-Pr-Tyr-D-Met-Gly-Phe-εAhx-OH (30) and H-iPrTyr-D-Met-Gly-Phe-εAhx-OH (31) have been synthesized and tested for agonistic, antagonistic and analgesic activity.Compound 24 showed a moderate μ agonistic potency and high selectivity.