Erectile Function Feeding Behavior--Obesity Pigmentation--Tanning Reproductive Ability Cardiovascular Function Learning Memory Immune Response HOT HOT.

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Presentation transcript:

Erectile Function Feeding Behavior--Obesity Pigmentation--Tanning Reproductive Ability Cardiovascular Function Learning Memory Immune Response HOT HOT Functions of  -MSH Analogues

Brief History of  -MSH Analogues

Synthesis of WY012 by SPPS

UGLY Facts related to Boc-(1-Me)His COST: US$645/g Synthesis Hydrophilicity assessed by HPLC (1’-Me)His and Boc-(1’-Me)His (Column dead volume is around 3.2 minutes)

Proposed Tactics--Using DIEA Salts

Reality of the Synthesis of DIEA Salts

HPLC Analysis of Crude Peptides Column: Vydac C 18 ; gradient: 10-90% A in 40 minutes [A: MeCN, B: (0.1% TFA) H 2 O]; flow: 1.0 mL; detection: 230, 254, 280 nm. a) From Boc-(1’-Me)His-OH; b) and c) From Boc-(1’-Me)-His DIEA and DIEA.HCl salts mix.

ConclusionsConclusions Mixture of Boc-(1’-Me)His.DIEA and DIEA.HCl salts was Successfully Applied to Peptide Syntheses This Method has Various Advantages, Including: Very Economic, Time-saving and Easy Access to Starting Materials This Method Should be Applicable to Other Hydrophilic Amino Acids

References and Acknowledgements 1. Eifler, S., Leblond, I., Trifilieff, E., and Lepoittevin, J.- P., Letters Pept. Sci., 4(1997) Pennington, M.W., and Dunn, B.M., (Eds.), Peptide Synthesis Protocols, Humana Press Inc., Miyazawa, T., Otomatsu, T.; Yamada, T.; Kuwata, S., Chem. Express, 4(1989) 745. US Public Health Service Funded by Grants From US Public Health Service Reprint: Contact: