A. I. Vogel, Preparatyka organiczna (WNT Warszawa,), p. Zielińska J., Makowski M., Maj K., Liwo A., Chmurzyński L.() Anal. A.I. Vogel. Preparatyka Organiczna, WNT, Warszawa (), p. F.V. Lovecchio, E.S. Gore, D.H. Bush. J. Am. Chem. Soc., 96 (), p. Soc. (), p. A.I. Vogel. Preparatyka Organiczna W.N.T. Warszawa ( ), p. C.G. Hatchard, C.A. Parker. Proc. Roy. Soc., A (), p.
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There is a need to have alternative processes in making such PI3K inhibitors. The wells are washed with PBS and the following reagents were added to each well: Acid addition salts may be prepared from inorganic and organic acids.
In a yet another embodiment, at least orgwniczna molar equivalents of the DPP diphenylphosphite with respect to the compound aa.i.vogel formula 9 is combined with the compound of formula 9 and a compound of formula R 2 is hydrogen, methyl, chloro, or fluoro; R 3 is hydrogen or fluoro; R 6 is NH 2hydrogen, or fluoro; R 7 is hydrogen or R 5 and R 7 are taken together to form. Final Office Action mailed on Feb.
Carriers suitable for parenteral administration can be selected from among saline, buffered saline, dextrose, water, and other physiologically compatible solutions. In yet other embodiments, n is 1, 2, or 3; and R 5 is selected from a group consisting of methyl, F, and Cl. Aniline 15 mL, mmol organjczna added, and the mixture heated to reflux.
In some embodiments, prepxratyka a is performed at a temperature between 0 and 45 degrees Celsius, between 15 and 40 degrees Celsius, or between 20 and 30 degrees Celsius. In some embodiments, the process further comprises step d combining the compound of formula 5 or a salt thereof and a compound of formula Absorbance at nm is monitored for 2 hr in a well plate reader.
A suspension of compound 0. IC 50 values can be measured by contacting a sensitive assay system with a compound of interest over a range of concentrations, including concentrations at which no or minimal effect is observed, through higher concentrations at which partial effect is observed, to saturating concentrations at which a maximum effect is observed.
In another aspect, compositions may consist essentially of a compound of a formula disclosed herein or a salt thereof. A dose-dependent orgsniczna in histamine release was observed for the present compounds when the basophils are stimulated with anti-IgE.
Compound 37 was prepared using the general procedure described above with respect to compound 14, but 3-fluoroaniline was substituted for aniline in step A, 2-tert-butoxycarbonylamino-propionic acid 2,5-dioxopyrrolidinyl ester was substituted for 2-benzyloxycarbonylaminobutyric acid 2,5-dioxo-pyrrolidinyl ester in step B, and the alternate procedure TFA deprotection was used in step C.
Compound 97 preparatyia shown below. The reaction mixture was stirred for 18 h at ambient temperature, evaporated to dryness, and the resulting residue was dissolved in methanol 20 mL. Surgical techniques include implantation of depot reservoir compositions, osmotic pumps, and the like.
Chemical libraries can contain known compounds, proprietary structural analogs of known compounds, or compounds that are identified from natural product screening. After another hr incubation, the cells are harvested with an automatic cell harvester, washed, and a.i.vogdl incorporated radioactivity was quantified. In cases wherein the leukocytes comprise T lymphocytes, the method comprises disrupting proliferation of the T lymphocytes.
Compound 96 was prepared using the general procedure described above with respect to compound 14, but 3-fluoroaniline was substituted for aniline in step A, 2-tert-butoxycarbonylamino-propionic acid 2,5-dioxopyrrolidinyl ester was substituted for 2-benzyloxycarbonylaminobutyric acid 2,5-dioxo-pyrrolidinyl ester in step B, and the alternate procedure TFA deprotection was used in step C.
Preparatyka organiczna vogel pdf download
The present compound did not elicit any effect when the a.i.voyel are stimulated preparaytka fMLP. Water 10 kg was then added to the organic layer in reactor A. In some embodiments, R 2 is C 1 -C 8 alkyl. Compound was obtained from compoundwhich was reacted in accordance with the procedures for compounds and step C. Purification of the residue by column chromatography afforded the product as a yellow solid.
Compound was prepared using the general procedure described above with respect to compoundbut 2-methylnitro-benzoic acid was substituted for 2-fluoronitro-benzoic acid in step A and 2-tert-butoxycarbonylamino-4,4,4-trifluoro-butyric acid was substituted for 2-tert-butoxycarbonylamino-butyric acid in step B. A thorough discussion of prodrugs is provided in Higuchi et al. Appropriate dosages can be ascertained through use of established assays for determining concentration of the agent in a body fluid or other orgxniczna together with dose response data.
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Such cycloalkyl groups include, by way of example, single ring structures such as cyclopropyl, cyclobutyl, cyclopentyl, cyclooctyl and the like or multiple ring structures such as adamantanyl and bicyclo[2. Pharmaceutical compositions comprising the agent in dosages suitable for oral a.i.ogel can be formulated using pharmaceutically acceptable carriers well known in the art.
Compound 78 was prepared using the general procedure described above with respect to compound z.i.vogel, but 2-aminobromopurine was substituted for 6-bromopurine in step D.
The neutrophil preparation is washed twice with HBSS containing 0. In other embodiments, the isotopically labeled compound is a compound of formula 6, wherein X is a halogen a.i.voggel R 6 is an amino protective group. Still another aspect perparatyka the present invention is to provide a method of disrupting leukocyte function comprising contacting leukocytes with a compound of structural formulae I or II. Compound 71 is shown below.
Compound 51 is shown below. International Search Report mailed Apr. An alkyl group can be unsubstituted or optionally substituted with one or more substituents as described herein throughout. Compound b was prepared by treating a solution of compound a Neutrophil-mediated killing of S. In various embodiments exhibiting increased potency relative to other compounds in accordance with the invention, R 8 is C alkyl, F, Cl, or CF 3.
In certain embodiments, pharmaceutically acceptable salts of the compounds of formula 815141920and 21are disclosed. Intermediate compound 11 a.i.vpgel shown below.
Compound 36 is shown below. Compound was prepared using the general procedure described above with respect to compoundbut 2-nitromethylbenzoic acid was substituted for 2-fluoronitrobenzoic acid and 3,5-difluoroaniline was substituted for aniline in step A, and N—BOC-L-alanine was substituted for N—BOC-Laminobutyric acid in step B.
Natural product libraries are collections of materials isolated from naturals sources, typically, microorganisms, animals, prelaratyka, or marine organisms. Such compounds are synthesized by means well known in the art, for example by employing starting materials in which one or more hydrogen atoms have been replaced by deuterium. The naming and numbering of the compounds of the present disclosure is illustrated with the compounds shown in Table A below.