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N-(1-oxopentyl)-N-[(2'(1-trityltetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl]-L-valine (TVS)

IP.com Disclosure Number: IPCOM000125347D
Publication Date: 2005-May-29
Document File: 2 page(s) / 107K

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N-(1-oxopentyl)-N-[(2'(1-trityltetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl]-L-valine (TVS)

N-(1-oxopentyl)-N-[(2'(1-trityltetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl]-L-valine (TVS) is used as an intermediate in the preparation of (S)-N-(1-Carboxy-2-methyl-prop-1-yl)-N- pentanoyl-N-[2'-(1H-tetrazol-5-yl)bi phenyl-4-ylmethyl]-amine (VLS).

Its chemical formula is:

  N N N

CH3

O

H3C OH

O

N

Bu

N

CPh3

Two different samples of TVS were examined by the XRD.

According to the XRD, TVS contains two different crystal forms: α and α-1. TVS Form α was supplied by Zhejiang Tianyu, and TVS Form α-1 was supplied by Zhejiang Huahai.

Form α may be identified by an X-ray powder diffraction pattern with peaks at: 5.3, 8.3, 10.8,
11.7, 12.3, 13.9, 18.3, 20.5, 21.7 and 24.6 degrees two-theta, ± 0.2 degrees two-theta.

Form α

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Form α-1 may be identified by an X-ray powder diffraction pattern with peaks at: 5.3, 6.5,
8.3, 9.5, 10.2, 10.8, 12.3, 13.5, 13.9, 18.3, 20.5, 21.7 and 24.6 degrees two-theta, ± 0.2 degrees two-theta.

X-Ray Powder Diffractions were performed on ARL (Scintag) X-Ray powder diffractometer model X'TRA, Cu-tube, solid state detector. A round standard aluminum sample holder with round zero background quartz plate was used. Scanning parameters: range 2-40 deg.2θ, continuous scan, rate 3 deg/min.

Form α-1