Synthesis of a Tyr3-octreotate conjugated closo-carborane [HC2B10H10]: A potential compound for boron neutron capture therapy

Tetrahedron Letters

Volumn 44, Issue 51, 2003, Pages 9143-9145

  Schirrmacher, Esther ^a   Schirrmacher, Ralf ^a   Beck, Carmen ^a   Mier, Walter ^b   Trautman, Norbert ^a   Rösch, Frank ^a  

^a JOHANNES GUTENBERG UNIVERSITY   (Germany)

^b UNIVERSITY HOSPITAL HEIDELBERG   (Germany)

Author keywords

Boron neutron capture therapy (BNCT); Closo carborane; Somatostatin receptor; Tyr3 octreotate

Indexed keywords

6,9 BIS(ACETONITRILE)DECABORANE; BORANE DERIVATIVE; CARBORANE DERIVATIVE; TYROSINE 3 OCTREOTATE CONJUGATED CLOSO CARBORANE; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL REACTION; DRUG SYNTHESIS; MATRIX ASSISTED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; NEUTRON CAPTURE THERAPY; PEPTIDE SYNTHESIS; PURIFICATION; REVERSED PHASE LIQUID CHROMATOGRAPHY; SOLID; SOLID STATE;

EID: 0345708159     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tetlet.2003.10.048     Document Type: Article

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20. t=24 min. The octreotate derivative 5 was a white solid after lyophilisation and the overall yield of the purified peptide was 17%.
21. 11B.
22. To establish the synthesis of 5 non-enriched decaborane (Alfa Aesar, Germany) was used. Highly enriched decaborane is commercially available and can be applied in the syntheses without modifications.