Abstract: The present invention aims to provide a more stable and efficient method for producing oligonucleotide, particularly, oligonucleotide having various functional groups linked to the 3?-terminal and the like.

Abstract: The focused ion beam apparatus includes: an ion source configured to generate ions; a first electrostatic lens configured to accelerate and focus the ions to form an ion beam; a beam booster electrode configured to accelerate the ion beam to a higher level; one or a plurality of electrodes, which are placed in the beam booster electrode, and are configured to electrostatically deflect the ion beam; a second electrostatic lens, which is provided between the one or plurality of electrodes and a sample table, and is configured to focus the ion beam applied with a voltage; and a processing unit configured to obtain a measurement condition, and set at least one of voltages to be applied to the one or plurality of electrodes or a voltage to be applied to each of the first electrostatic lens and the second electrostatic lens, based on the obtained measurement condition.

Abstract: Disclosed is a composite charged particle beam apparatus including: an ion supply unit supplying an ion beam; an acceleration voltage application unit applying an acceleration voltage to the ion beam supplied by the ion supply unit to accelerate the ion beam; a first focusing unit focusing the ion beam; a beam booster voltage application unit applying a beam booster voltage to the ion beam; a second focusing unit focusing the ion beam to irradiate a sample; an electron beam emission unit emitting an electron beam to irradiate the sample; and a controller setting a value of the beam booster voltage that the beam booster voltage application unit applies to the ion beam, based on a value of the acceleration voltage applied to the ion beam by the acceleration voltage application unit and of a set value predetermined according to a focal distance of the focused ion beam.

Abstract: The focused ion beam apparatus includes: an ion source configured to generate ions; a first electrostatic lens configured to accelerate and focus the ions to form an ion beam; a beam booster electrode configured to accelerate the ion beam to a higher level; one or a plurality of electrodes, which are placed in the beam booster electrode, and are configured to electrostatically deflect the ion beam; a second electrostatic lens, which is provided between the one or plurality of electrodes and a sample table, and is configured to focus the ion beam applied with a voltage; and a processing unit configured to obtain a measurement condition, and set at least one of voltages to be applied to the one or plurality of electrodes or a voltage to be applied to each of the first electrostatic lens and the second electrostatic lens, based on the obtained measurement condition.

Abstract: Oligonucleotides may be produced by a process, including (1) condensing a nucleoside, nucleotide or oligonucleotide (b), and a nucleoside, nucleotide or oligonucleotide (a), or a substituted nucleotide or oligonucleotide (?) in a non-polar solvent to give a reaction solution containing a phosphite triester product (c); (3) oxidizing or sulfurizing the phosphite triester product (c) to give a reaction solution containing an oligonucleotide (d) wherein the 5?-hydroxy group is protected; (4) deprotecting the oligonucleotide (d) to give a reaction solution containing an oligonucleotide (e) wherein the 5?-hydroxy group is not protected; and (6) adding a polar solvent to the reaction solution containing the oligonucleotide (e) and purifying the oligonucleotide (e) by solid-liquid separation, wherein said nucleoside, nucleotide or oligonucleotide (a) or said substituted nucleotide or oligonucleotide (?) is a compound represented by formula (a-i): wherein Base, Rp1, R10, m, L, Y, and Z are defined herein.

Abstract: Disclosed is a composite charged particle beam apparatus including: an ion supply unit supplying an ion beam; an acceleration voltage application unit applying an acceleration voltage to the ion beam supplied by the ion supply unit to accelerate the ion beam; a first focusing unit focusing the ion beam; a beam booster voltage application unit applying a beam booster voltage to the ion beam; a second focusing unit focusing the ion beam to irradiate a sample; an electron beam emission unit emitting an electron beam to irradiate the sample; and a controller setting a value of the beam booster voltage that the beam booster voltage application unit applies to the ion beam, based on a value of the acceleration voltage applied to the ion beam by the acceleration voltage application unit and of a set value predetermined according to a focal distance of the focused ion beam.

Abstract: Precipitation promoters, which are an organic compound having one or more linear aliphatic hydrocarbon groups having not less than 10 carbon atoms, wherein the aliphatic hydrocarbon group has not less than 20 carbon atoms in total are useful for precipitating an organic compound protected by an organic group having one or more aliphatic hydrocarbon groups having not less than 10 carbon atoms from a solvent.

Abstract: The present invention aims to provide a more stable and efficient method for producing oligonucleotide, particularly, oligonucleotide having various functional groups linked to the 3?-terminal and the like.

Abstract: Oligonucleotides may be produced by a process, including (1) condensing a nucleoside, nucleotide or oligonucleotide (a) or the like wherein a 5?-hydroxy group is not protected and a nucleoside, nucleotide or oligonucleotide (b) wherein a 5?-hydroxy group is protected in a non-polar solvent to give a reaction solution containing a phosphite triester product (c); (3) oxidizing or sulfurizing the phosphite triester product (c) to give a reaction solution containing an oligonucleotide (d) wherein the 5?-hydroxy group is protected; (4) deprotecting the oligonucleotide (d) to give a reaction solution containing an oligonucleotide (e) wherein the 5?-hydroxy group is not protected; and (6) adding a polar solvent to the reaction solution containing the oligonucleotide (e) and purifying the oligonucleotide (e) by solid-liquid separation or extraction.

Abstract: Precipitation promoters, which are an organic compound having one or more linear aliphatic hydrocarbon groups having not less than 10 carbon atoms, wherein the aliphatic hydrocarbon group has not less than 20 carbon atoms in total are useful for precipitating an organic compound protected by an organic group having one or more aliphatic hydrocarbon groups having not less than 10 carbon atoms from a solvent.

Abstract: Highly pure (2R,3S)-3-tert-butoxycarbonylamino-1-chloro-2-hydroxy-4-phenylbutane or (2S,3R)-3-tert-butoxycarbonylamino-1-chloro-2-hydroxy-4-phenylbutane may be conveniently produced in high yield by: (a) reacting compound (1) with lithiumchloromethane to give compound (2) and at least a byproduct; (b) dissolving compound (2) and the byproduct in a polar solvent and adding water to the solution to precipitate compound (2) as crystals; (c) reducing the crystals of compound (2) to give compound (3) and at least its diastereomer as an impurity; (d) adding sulfuric acid thereto to give compound (4) and at least its diastereomer as an impurity; and (e) precipitating compound (4) as crystals from a solution containing acetic acid ester or acetic acid ester.

Abstract: Herein are disclosed a process for increasing in purity, or purifying, an N-protected-?-aminoalcohol which process comprises (i) adding water to a polar organic solvent in which an N-protected-?-aminoalcohol such as a (2R,3S)- or (2S,3R)-3-tert-butoxycarbonylamino-1-halo-2-hydroxy-4-phenylbutane or the like, or (ii) crystallizing such an N-protected-?-aminoalcohol from a diol or a diol-based mixed solvent, and a process for producing the corresponding N-protected-?-aminoepoxide which process comprises treating, with a base, the thus purity-enhanced N-protected-?-aminoalcohol. Such N-protected-?-aminoalcohols and N-protected-?-aminoepoxides are both useful as synthetic intermediates for medicine compounds, such as, e.g., HIV protease inhibitor and the like.

Abstract: A process for producing ?-aminohalomethyl ketones or N-protected ?-aminohalomethyl ketones from specified 3-oxazolidin-5-one derivatives via 5-halomethyl-5-hydroxy-3-oxazolidine derivatives. By this process, ?-aminohalomethyl ketones and compounds relating to them can be obtained efficiently and economically in industrial scale.

Abstract: The present invention relates to a method of producing a highly pure crystal, which includes crystallization of a benzenesulfonamide derivative of the following formula (1) using a polar solvent as a good solvent (e.g.

Abstract: Herein are disclosed a process for increasing in purity, or purifying, an N-protected-&bgr;-aminoalcohol which process comprises (i) adding water to a polar organic solvent in which an N-protected-&bgr;-aminoalcohol such as a (2R,3S)-or (2S,3R)-3-tert-butoxycarbonylamino-1-halo-2-hydroxy-4-phenylbutane or the like, or (ii) crystallizing such an N-protected-&bgr;-aminoalcohol from a diol or a diol-based mixed solvent, and a process for producing the corresponding N-protected-&bgr;-aminoepoxide which process comprises treating, with a base, the thus purity-enhanced N-protected-&bgr;-aminoalcohol. Such N-protected-&bgr;-aminoalcohols and N-protected-&bgr;-aminoepoxides are both useful as synthetic intermediates for medicine compounds, such as, e.g., HIV protease inhibitor and the like.

Abstract: A process for producing &agr;-aminohalomethyl ketones or N-protected &agr;-aminohalomethyl ketones from specified 3-oxazolidin-5-one derivatives via 5-halomethyl-5-hydroxy-3-oxazolidine derivatives. By this process, &agr;-aminohalomethyl ketones and compounds relating to them can be obtained efficiently and economically in industrial scale.

Abstract: The invention relates to a method for industrially producing highly pure (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide (crystal) or (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoalcohol.

Abstract: The present invention provides a production method including adding water to a solution of (2R,3S)-3-tert-butoxycarbonylamino-1,2-epoxy-4-phenylbutane ((2R,3S)-epoxide compound) or (2S,3R)-3-tert-butoxycarbonylamino-1,2-epoxy-4-phenylbutane ((2S,3R)-epoxide compound) in a polar solvent to allow crystallization, whereby to produce crystals of the (2R,3S)-epoxide compound or the (2S,3R)-epoxide compound conveniently in a high yield by an industrial production method without requiring an extremely low temperature.

Abstract: A process for producing &agr;-aminohalomethyl ketones or N-protected &agr;-aminohalomethyl ketones from specified 3-oxazolidin-5-one derivatives via 5-halomethyl-5-hydroxy-3-oxazolidine derivatives. By this process, &agr;-aminohalomethyl ketones and compounds relating to them can be obtained efficiently and economically in industrial scale.

Abstract: An amino group of an &agr;-amino acid ester is protected as an imine, and it is then reacted with a halomethyllithium to obtain an N-protected-&agr;-aminohalomethylketone. Further, this N-protected-&agr;-aminohalomethylketone is treated with an acid to obtain an &agr;-aminohalomethylketone. This process is suited for industrial production, and can produce an &agr;-aminohalomethylketone and its related compounds economically and efficiently.