Abstract: A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Abstract: A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Abstract: A process for preparation of a compound of formula I: wherein: R1 represents CH3 or H; and P represents a protecting group; comprising reacting a compound of formula IV:  wherein R1 and P and are defined above and R4 represents triflate or SO2F; in the presence of a catalyst and (R3)3SnCH2OP″, wherein each R3 represents C1-4 lower alkyl, and P″ represents H or a protecting group, to yield the compound of formula I.

Abstract: Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.

Abstract: A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Abstract: A process of synthesizing a carbapenem compound of formula 6: is disclosed using a compound of formula 4′: The intermediate compounds that are described herein are also included in the present invention.

Abstract: The invention describes an improved process for synthesizing 1-&bgr;-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The synthesis eliminates the use of BU3SnCH2OH and HMPA, which are toxic substances and not amenable to industrial scale production. The novel intermediates are also within the scope of this invention. The invention relates to the synthesis of a compound of formula 3: wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents H or methyl; and R5 represents a carboxy protecting group as well as the compounds made therein.

Abstract: Novel crystalline carbapenem intermediate compounds of formula I: ##STR1## wherein: R.sub.1 represents CH.sub.3 or H and an efficient process for synthesis thereof are described.

Abstract: A method of and a device for positioning an area of a living body to be measured relative to a detecting probe during a biodata measurement with the use of a biodata measuring apparatus designed to irradiate with light the area of the living body by means of the detecting probe then held in contact with the area of the living body, then to detect light transmitted through and/or reflected from the area of the living body, and finally to measure a predetermined biodata within the living body on the basis of a spectrum of the transmitted and/or reflected light. A plurality of local fixing units are utilized for fixing a plurality of predetermined portions of the living body, respectively. The portions of the living body are fixed respectively by the local fixing units during the biodata measurement to thereby fix the area to be measured relative to the positioning device.

Abstract: A process of synthesizing a compound of formula I is described: ##STR1## wherein P and P' independently represent H or a protecting group, R.sub.1 represents H or C.sub.1-4 alkyl, and Hal represents a halogen characterized by reacting a compound of formula 2: ##STR2## with R.sub.2 OH, wherein R.sub.2 is C.sub.1-4 alkyl, C.sub.6-10 aryl or C.sub.5-10 heteroaryl in the presence of an acid catalyst or carbodiimide reagent to produce a compound of formula 3: ##STR3## and reacting a compound of formula 3 in the presence of a base and a haloalkylating agent to produce a compound of formula 1.

Abstract: A method of and an apparatus for regulating a pressure applied to an area of a living body during a biodata measurement with the use of a biodata measuring apparatus. The apparatus is designed to irradiate with light the area of the living body by means of a detecting probe then held in contact with the area of the living body, then to detect light transmitted through and/or reflected from the area of the living body, and finally to measure a predetermined biodata within the living body on the basis of a spectrum of the transmitted and/or reflected light. The method and the apparatus include pressing, during the biodata measurement, the area of the living body with a predetermined pressure through a soft pressure medium to thereby regulate the pressure applied to the area of the living body to a value equal to the predetermined pressure.

Abstract: The present invention relates to a process for synthesizing novel intermediates of formula III: ##STR1## wherein R.sup.1 is a halogen. The intermediate compounds described herein are useful for the preparation of carbapenem compounds.

Abstract: A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.

Abstract: A process of synthesizing a compound of formula 1: ##STR1## wherein P and P' each independently represent H or a protecting group, R.sup.1 represents H or C.sub.1-4 alkyl, andHal represents a halogen selected from Cl, Br and I, comprising: reacting a compound of formula 2: ##STR2## wherein P, P' and R.sub.1 are as defined above with an N,O-di-C.sub.1-4 alkyl hydroxylamine in the presence of a carbodiimide to produce a compound of formula 3: ##STR3## reacting compound 3 with a compound of formula 4:MetCH.sub.2 SiR.sub.2 R.sub.3 R.sub.4 4wherein Met represents lithium or halomagnesium;R.sub.2, R.sub.3 and R.sub.4 are C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and the halo portion of halomagnesium is Cl, Br or I, to produce a compound of formula 5: ##STR4## and reacting compound 5 with a halogenating agent to produce a compound of formula 1.

Abstract: The invention encompasses a method for the stereoselective synthesis of alkyl proline and other amino acid derivatives which are intermediates of the farnesyl-protein transferase inhibiting CA.sup.1 A.sup.2 X motif of the protein Ras. The instant process employs an efficient diastereoselective ?2,3!-Wittig rearrangement of .alpha.-allyloxy amide enolates mediated by a chiral auxiliary to provide acyclic and cyclic precursors.

Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.

Abstract: A chiral resolution process is described for the purification of a substituted chiral quinazoline, by salt formation with a resolving agent, followed by crystallization.

Abstract: The present invention is directed to a process of making 2-Aryl Carbapenems of Formula 1 from a compound of formula 2.