- Reagents for Efficient Conversion of Amines to Protected Guanidines
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Two new guanidinylation reagents, N,N′-bis(ortho-chloro-Cbz)-S- methylisothiourea and N,N′-bis(ortho-bromo-Cbx)-S-methylisothiourea, were compared with the already known N,N′-bis(Boc)-S-methylisothiourea and N,N′-bis(Cbz)-S-methylisothiourea. The new reagents proved to be superior to the known reagents. The reactions with all the new reagents were accelerated by addition of DMAP. N,N′-Bis(ortho-chloro-Cbz)- and N,N′-bis(ortho- bromo-Cbz)guanidines are stable when treated with trifluoroacetic acid and can be converted to guanidines by hydrogenolysis.
- Gers, Tomasz,Kunce, Danuta,Markowski, Pawe?,Izdebski, Jan
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- Selective carbamate conversion of protected guanidines
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The reactivity of carbamates to produce other carbamates (by reaction with alcohols) or amidinoureas (by reaction with amines), without the use of strong bases or catalysts, has been studied indicating the suitability/selectivity of the method in achievin
- Rahman, Adeyemi,Stipani?ev, Nikolina,Keogh, Aaron P.,Twamley, Brendan,Rozas, Isabel
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- IMAGE-GUIDED ENERGY DEPOSITION FOR TARGETED DRUG DELIVERY
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Disclosed are compositions and methods for targeted drug delivery using image-guided energy deposition to help localize active compounds to particular sites within the body of an animal. Also provided are compounds and formulations thereof for use in the
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- THIOPHENE -2- CARBOXYLIC ACID - (1H - BENZIMIDAZOL - 2 YL) - AMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE TEC KINASE ITK (INTERLEUKIN -2- INDUCIBLE T CELL KINASE) FOR THE TREATMENT OF INFLAMMATION, IMMUNOLOGICAL AND ALLERGIC DISORDERS
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Disclosed are compounds of formula (I): wherein Ar1, Ar2, R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for
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Page/Page column 129
(2010/02/13)
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- Compounds with antiparasitic activity and medicines containing same
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The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.
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Page/Page column 6
(2008/06/13)
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- Efficient synthesis of (S)-(-)- and (R)-(+)-enantiomers of 15-deoxyspergualin (15-DSG)
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An efficient synthesis of the (S)-(-)- and (R)-(+)-enantiomers of 15-deoxyspergualin (15-DSG) is reported. The synthesis involves preparative HPLC separation and subsequent hydrogenolysis of two diastereoisomers 10a and 10b of fully protected 15-DSG penultimates. Alternatively, diastereomerically pure amide 10b (97% de) was also prepared from acid 8b (97% de), which was obtained via crystallization of a 1:1 diastereomeric mixture of 8a and 8b. Copyright (C) 2000 Elsevier Science Ltd.
- Wang, Xuebao,Thottathil, John
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p. 3665 - 3669
(2007/10/03)
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- ANTITHROMBOTIC AGENTS
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This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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- Preparation of optically active (S)-(-) and (R)-(+)-deoxyspergualin and novel intermediates thereof
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A process for preparing optically active (S)-(-) and (R)-(+)-deoxyspergualin and salts thereof of the formula I STR1 by reacting a compound of formula II STR2 with a compound of formula III STR3 in the presence of a condensing/dehydrating agent and an org
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- ANTITHROMBOTIC AGENTS
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This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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- ANTITHROMBOTIC AGENTS
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This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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- ANTITHROMBOTIC AGENTS
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This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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- ANTITHROMBOTIC AGENTS
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This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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- A practical synthesis of free and protected guanidino acids from amino acids
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Synthesis of protected guanidino acids in one pot reaction is achieved. Amino acids are treated with trimethylsilyl chloride, triethylamine, dicarbobenzoxy-S-methyl isothiourea in dichloromethane followed by removal of silyl group by treatment with methanol to give the corresponding carbobenzoxy guanidino acids.
- Lal, Bansi,Gangopadhyay
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p. 2483 - 2486
(2007/10/03)
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