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249921-19-5

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A practical synthesis of the pseudotripeptide RC-1291
The rapid process development of a scaleable synthesis of the pseudotripeptide RC-1291 for preclinical and clinical evaluation is described. By employing a nontraditional N-to-C coupling strategy, the peptide chain of RC-1291 was assembled in high yield, with minimal racemization and in an economical manner by introducing the most expensive component last. A one-pot deprotection/crystallization procedure was developed for the isolation of RC-1291 free base, which afforded the target compound in excellent yield and with a purity of >99.5% without chromatographic purification.
Paul, Bernhard J.,Littler, Benjamin J.,Jos, Frederic,Vogt, Paul F.,Pines, Seemon H.
p. 339 - 345
(2012/12/22)

CRYSTAL FORMS OF (3R)-1-(2-METHYLALANYL-D-TRYPTOPHYL)-3-(PHENYLMETHYL)-3-PIPERIDINECARBOXYLIC ACID 1,2,2-TRIMETHYLHYDRAZIDE
Crystalline polymorphs of (3 R)-1-(2-methylalanyl-D-tryptophyl)-3- (phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone.
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Page/Page column 30

(2008/06/13)

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Chemical Properties

Density: 1.214
Solubility:DMSO (Slightly), Methanol (Slightly)
Storage Temp.:Refrigerator
PKA: 16.22±0.46(Predicted)
PSA: 114.77000
LogP: 3.74810

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