Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl

Base Information

• Chemical Name: Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl
• CAS No.: 102410-63-9
• Molecular Formula: C₅₀H₅₇N₇O₁₁*2ClH
• Molecular Weight: 1004.96
• Mol file: 102410-63-9.mol

Synonyms:

Chemical Property of Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl

Chemical Property:

Purity/Quality:

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

Technology Process of Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl

There total 21 articles about Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

proline tert-butyl ester (2812-46-6) → Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl (102410-63-9)

Guidance literature:

Multi-step reaction with 7 steps

1: 100 percent / EDCI, HOBt, NMM / CH₂Cl₂ / 1.) 4 h from -15 deg C to room temp., 2.) 2 d, room temp.

2: 96 percent / H₂ / 5percent Pd/C / methanol / 12 h / Ambient temperature

4: 93 percent / PPA, DMAP, NMM / CH₂Cl₂ / 1.) 2 h, -15 to -10 deg C, 2.) 6 d, -2 deg C

5: 100 percent / Et₂NH / CH₂Cl₂ / 3 h / Ambient temperature

6: 64 percent / EDCI, DMAP, NMM / CH₂Cl₂ / 1.) 4 h, -15 deg C to room temp., 2.) 2 d, room temp.

7: 100 percent / 6 N HCl / CH₂Cl₂; dioxane / 4 h / Ambient temperature

With 4-methyl-morpholine; hydrogenchloride; dmap; hydrogen; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; diethylamine; palladium on activated charcoal; In 1,4-dioxane; methanol; dichloromethane;

DOI:10.1002/jlac.198619860101

Reference yield:

Z-D-Abu-Pro-OBut (102410-49-1) → Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl (102410-63-9)

Guidance literature:

Multi-step reaction with 6 steps

1: 96 percent / H₂ / 5percent Pd/C / methanol / 12 h / Ambient temperature

3: 93 percent / PPA, DMAP, NMM / CH₂Cl₂ / 1.) 2 h, -15 to -10 deg C, 2.) 6 d, -2 deg C

4: 100 percent / Et₂NH / CH₂Cl₂ / 3 h / Ambient temperature

5: 64 percent / EDCI, DMAP, NMM / CH₂Cl₂ / 1.) 4 h, -15 deg C to room temp., 2.) 2 d, room temp.

6: 100 percent / 6 N HCl / CH₂Cl₂; dioxane / 4 h / Ambient temperature

With 4-methyl-morpholine; hydrogenchloride; dmap; hydrogen; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; diethylamine; palladium on activated charcoal; In 1,4-dioxane; methanol; dichloromethane;

DOI:10.1002/jlac.198619860101

Reference yield:

Pic(3-OBzl)-OH*HCl (5603-02-1) → Pic(3-OBzl)-Thr(H-MePhe-4Kps-Phg-)-D-Abu-Pro-OH*2HCl (102410-63-9)

Guidance literature:

Multi-step reaction with 7 steps

1: 76 percent / PPA, NMM / CH₂Cl₂ / 1.) 4 h, -15 deg C to room temp., 2.) 2 d, room temp.

2: 81 percent / PPA, DMAP, NMM / CH₂Cl₂ / 1.) 2 h, -15 to -10 deg C, 2.) 6 d, -2 deg C

3: 81 percent / 6.5 N HCl / dioxane / 4 h / Ambient temperature

4: 39 percent / PPA, NMM / CH₂Cl₂ / 1.) 4 h, -15 deg C to room temp., 2.) 2 d, room temp.

5: 100 percent / Et₂NH / CH₂Cl₂ / 3 h / Ambient temperature

6: 64 percent / EDCI, DMAP, NMM / CH₂Cl₂ / 1.) 4 h, -15 deg C to room temp., 2.) 2 d, room temp.

7: 100 percent / 6 N HCl / CH₂Cl₂; dioxane / 4 h / Ambient temperature

With 4-methyl-morpholine; hydrogenchloride; dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; diethylamine; In 1,4-dioxane; dichloromethane;

DOI:10.1002/jlac.198619860101

upstream raw materials:

Boc-N-Me-Phe-OH

proline tert-butyl ester

Pic(3-OBzl)-ONp

N-benzyloxycarbonyl-(2S,4R)-4-hydroxypipecolic acid

Downstream raw materials:

3-Benzyloxy-pyridine-2-carboxylic acid ((3S,6S,15S,16R,22S)-3-benzyl-12-ethyl-4,16-dimethyl-2,5,11,14,18,21,24-heptaoxo-19-phenyl-17-oxa-1,4,10,13,20-pentaaza-tricyclo[20.4.0.0^6,10]hexacos-15-yl)-amide