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A new synthesis of deglyco-bleomycin A2 aiming at the total synthesis of bleomycin

โœ Scribed by Sei-ichi Saito; Yoji Umezawa; Hajime Morishima; Tomohisa Takita; Hamao Umezawa; Masatoshi Narita; Masami Otsuka; Susumu Kobayashi; Masaji Ohno

Book ID
104220380
Publisher
Elsevier Science
Year
1982
Tongue
French
Weight
202 KB
Volume
23
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

An improved route to synthesize deglyco-bleomycin A2, the aglycon of bleomycin A2, aiming at the total synthesis of bleomycin is described. The new route is characterized by the stepwise elongation of the amino acid constituents and the use of a thiol ester obtained by aldol condensation.

Deglyco-bleomycin A2, the aglycon of bleomycin (BLM) A2, is a hexapeptide consisting of five amino acids and a terminal amine 1) . Deglyco-BLM was found in the culture broth in a trace amount and also isolated from the mild acid hydrolyzate of BLM 2)

  1. . The first total synthesis of deglyco-BLM A2 , achieved by us, was based on the fragment condensation of the dipeptide (;t-z) and tripeptide S 3, (2) followed by coupling with pyrimidoblamic acid (4).

๐Ÿ“œ SIMILAR VOLUMES

Total synthesis of deglyco-bleomycin A2
Total synthesis of deglyco-bleomycin A2
โœ Tomohisa Takita; Yoji Umezawa; Sei-ichi Saito; Hajime Morishima; Hamao Umezawa; ๐Ÿ“‚ Article ๐Ÿ“… 1981 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 235 KB

Surmnary: Deglyco-bleomycin A2, the aglycon of bleomycin time. A2, has been synthesized for the first Bleomycin (BIM) is an antitumor antibiotic clinically used in the treatment of squamous cell carcinoma and malignant lymphoma. 1 In addition to its medicinal importance, BLM is of great interest bec

Total synthesis of bleomycin A21)
Total synthesis of bleomycin A21)
โœ Tomohisa Takita; Yoji Umezawa; Sei-ichi Saito; Hajime Morishima; Hiroshi Naganaw ๐Ÿ“‚ Article ๐Ÿ“… 1982 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 231 KB

Bleomycin A2 has been synthesized for the first time. Bleomycin (BLM) is an antitumor antibiotic clinically used in the treatment of squamous cell carcinoma, malignant lymphoma and testis tumors. BLM A2 (Q2), the major component of natural BLMs, consists of a linear hexapeptide named deglyco-BLM A2